Imatinib

别名: STI571, CGP-57148B 中文名称:伊马替尼

Imatinib是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。

Imatinib Chemical Structure

Imatinib Chemical Structure

CAS: 152459-95-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 746.33 现货
250mg RMB 571.38 现货
1g RMB 1613.43 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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客户使用Selleck的Imatinib发表文献300

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批次: 纯度: 99.97%
99.97

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相关信号通路图

PDGFR抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
BA/F3 Antiproliferative assay 5 to 10 uM 48 hrs Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.055μM. 16415863
BA/F3 Antiproliferative assay 5 to 10 uM 48 hrs Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH3-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.088μM. 16415863
BA/F3 Antiproliferative assay 5 to 10 uM 48 hrs Antiproliferative activity against mouse BA/F3 cells expressing NPM-abl assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.393μM. 16415863
Ba/F3 Function assay 1 uM 24 hrs Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as release of full-length c-Abl from cytoplasmic complex with 14-3-3sigma at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique 21962576
Ba/F3 Function assay 1 uM 24 hrs Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as nuclear import of full-length c-Abl at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique 21962576
K562 Function assay 40 uM 6 hrs Inhibition of BCR-ABL-mediated ERK1 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry 22148584
K562 Function assay 40 uM 6 hrs Inhibition of BCR-ABL-mediated ERK2 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry 22148584
HEK293 Function assay 500 uM 1.5 mins Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay, IC50=0.35μM. 23241029
BA/F3 Antitumor assay 50 mg/kg 14 days Antitumor activity against mouse BA/F3 cells expressing wild type BCR-ABL allografted in SCID mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 14 days 23301703
K562 Function assay 10 uM 1 hr Inhibition of Bcr/Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis 24681986
K562 Function assay 10 uM 1 hr Inhibition of Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis 24681986
K562 Function assay 10 uM 1 hr Inhibition of tyrosine phosphorylation of protein with molecular weight between 40 and 60 kDa in human K562 cells at 10 uM after 1 hr by immunoblot analysis 24681986
K562 Function assay 100 uM 8 hrs Inhibition of BCR-ABL signaling pathway in human K562 cells assessed as suppression of STAT5 phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis 27666635
K562 Function assay 100 uM 8 hrs Inhibition of BCR-ABL in signaling pathway human K562 cells assessed as suppression of CrkL phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis 27666635
K562 Function assay 100 uM 8 hrs Inhibition of BCR-ABL phosphorylation in human K562 cells at 100 uM after 8 hrs in presence of MeBS by Western blot analysis 27666635
K562 Cell cycle assay 1 uM 24 hrs Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry 27966954
KU812 Cell cycle assay 1 uM 12 hrs Cell cycle arrest in human KU812 cells assessed as accumulation at G0/G1 phase at 1 uM after 12 hrs by propidium iodide/RNase staining based flow cytometry 27966954
MEG01 Cell cycle assay 1 uM 24 hrs Cell cycle arrest in human MEG01 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry 27966954
GISTT1 Cell cycle assay 1 uM 24 hrs Cell cycle arrest in human GISTT1 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry 27966954
GIST882 Cell cycle assay 1 uM 48 hrs Cell cycle arrest in human GIST882 cells assessed as accumulation at G0/G1 phase at 1 uM after 48 hrs by propidium iodide/RNase staining based flow cytometry 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y703 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y719 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y823 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y703 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y719 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT autophosphorylation at Y823 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GISTT1 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
GIST882 Function assay 1 uM 2 hrs Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 27966954
NCI-H1703 Function assay 1 uM 2 hrs Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y1018 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis 29544149
NCI-H1703 Function assay 1 uM 2 hrs Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y754 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis 29544149
NCI-H1703 Function assay 1 uM 2 hrs Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y849 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis 29544149
EOL-1 Function assay 1 uM 2 hrs Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in STAT5 phosphorylation at Y694 residue at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis 29544149
EOL-1 Function assay 1 uM 2 hrs Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in ERK phosphorylation at T202/Y204 residues at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis 29544149
K562 Apoptosis assay 10 uM 48 hrs Induction of apoptosis in human K562 cells assessed as increase in apoptotic cells at 10 uM incubated for 48 hrs by Caspase-3/7 reagent-based fluorescence assay 31097376
Neuro2a Function assay 1 uM Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
K562 Apoptosis assay 1 uM Induction of apoptosis in human K562 cells assessed as cleavage of PARP at 1 uM by Western blot analysis 27966954
K562 Apoptosis assay 1 uM Induction of apoptosis in human K562 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis 27966954
KU812 Apoptosis assay 1 uM Induction of apoptosis in human KU812 cells assessed as cleavage of PARP at 1 uM by Western blot analysis 27966954
KU812 Apoptosis assay 1 uM Induction of apoptosis in human KU812 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis 27966954
MEG01 Apoptosis assay 1 uM Induction of apoptosis in human MEG01 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis 27966954
GISTT1 Apoptosis assay 1 uM Induction of apoptosis in human GISTT1 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis 27966954
MEG01 Apoptosis assay 1 uM Induction of apoptosis in human MEG01 cells assessed as cleavage of PARP at 1 uM by Western blot analysis 27966954
GISTT1 Apoptosis assay 1 uM Induction of apoptosis in human GISTT1 cells assessed as cleavage of PARP at 1 uM by Western blot analysis 27966954
GIST882 Apoptosis assay 1 uM Induction of apoptosis in human GIST882 cells assessed as cleavage of PARP at 1 uM by Western blot analysis 27966954
GIST882 Apoptosis assay 1 uM Induction of apoptosis in human GIST882 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis 27966954
K562 Function assay 1 uM Inhibition of BCR-ABL in imatinib-sensitive human K562 cells assessed as decrease in CrKL phosphorylation at 1 uM by immuno blot analysis 30261468
BA/F3 Antiproliferative assay 48 hrs Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay, IC50=0.027μM. 16415863
32D Antiproliferative assay 48 hrs Antiproliferative activity against mouse 32D cells transfected with p210 cells expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50=0.112μM. 16415863
BA/F3 Antiproliferative assay 48 hrs Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay, IC50=0.19μM. 16415863
BA/F3 Antiproliferative assay 48 hrs Antiproliferative activity against mouse BA/F3 cells transfected with p210 Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50=0.19μM. 16415863
M07e Antiproliferative assay 48 hrs Antiproliferative activity against human M07e Bcr-abl negative cells expressing stem cell factor assessed as proliferation after 48 hrs by MTT assay, IC50=0.257μM. 16415863
BA/F3 Antiproliferative assay 48 hrs Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay, IC50=0.339μM. 16415863
BA/F3 Antiproliferative assay 48 hrs Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay, IC50=0.962μM. 16415863
Vero Antiviral assay 3 days Antiviral activity against Dengue virus infected in african green monkey Vero cells administered before viral challenge after 3 days by viral plaque assay 17360676
EOL-1 Cytotoxicity assay 72 hrs Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.0001995μM. 19301902
EOL-1 Cytotoxicity assay 72 hrs Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.0002μM. 19301902
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.049μM. 19301902
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.1μM. 19301902
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by alamar-blue cell viability assay, IC50=10μM. 19301902
RKOp21 Cytotoxicity assay 72 hrs Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50=12μM. 19301902
RKOp21 Cytotoxicity assay 72 hrs Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50=12.5892μM. 19301902
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50=15.5μM. 19301902
MDA-MB-468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50=15.8489μM. 19301902
MDA-MB-468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50=17μM. 19301902
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50=18.65μM. 19301902
Hec1A Cytotoxicity assay 72 hrs Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50=19μM. 19301902
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM. 19301902
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM. 19301902
Hec1A Cytotoxicity assay 72 hrs Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM. 19301902
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50=22μM. 19301902
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50=24μM. 19301902
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50=24μM. 19301902
HCT15 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50=25μM. 19301902
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM. 19301902
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM. 19301902
HCT15 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM. 19301902
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM. 19301902
Saos2 Cytotoxicity assay 72 hrs Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM. 19301902
Saos2 Cytotoxicity assay 72 hrs Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50=26μM. 19301902
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50=30μM. 19301902
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50=31μM. 19301902
H69 Cytotoxicity assay 72 hrs Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM. 19301902
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM. 19301902
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM. 19301902
H69 Cytotoxicity assay 72 hrs Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50=32μM. 19301902
CCRF-CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50=36μM. 19301902
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM. 19301902
CCRF-CEM/VCR1000 Cytotoxicity assay 72 hrs Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM. 19301902
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM. 19301902
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50=38μM. 19301902
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50=39μM. 19301902
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
AsPC1 Cytotoxicity assay 72 hrs Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
CCRF-CEM/VCR1000 Cytotoxicity assay 72 hrs Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
CCRF-CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM. 19301902
AsPC1 Cytotoxicity assay 72 hrs Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50=44μM. 19301902
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by alamar-blue cell viability assay, IC50=48μM. 19301902
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50=0.06μM. 19469547
GIST882 Antiproliferative assay 96 hrs Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay, IC50=1.7μM. 19469547
HGC27 Antiproliferative assay 96 hrs Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50=2.4μM. 19469547
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50=11.5μM. 19469547
GIST48 Cytotoxicity assay 3 to 6 days Cytotoxicity against human GIST48 cells assessed as effect on cell viability after 3 to 6 days by luciferase based luminescence assay, IC50=18.7μM. 19469547
KBM5 Cytotoxicity assay 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTT assay, IC50=0.28μM. 20149665
KBM5 Cytotoxicity assay 72 hrs Cytotoxicity against human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTT assay, IC50=5.4μM. 20149665
FDC-P1 Function assay 48 hrs Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50=1.274μM. 20156689
FDC-P1 Function assay 48 hrs Inhibition of mouse GM-CSF-stimulated cell proliferation of growth factor dependent mouse FDC-P1 cells expressing human FMS after 48 hrs by resazurin dye reduction assay, IC50=8.437μM. 20156689
K562 Function assay 2 hrs Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis, IC50=0.75μM. 20188579
BESM Antitrypanosomal assay 88 hrs Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=9μM. 20547819
BESM Cytotoxicity assay 88 hrs Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM. 20547819
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=0.58μM. 21295380
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=5.4μM. 21576023
K562 Function assay 6 hrs Inhibition of BCR-ABL-mediated STAT5 phosphorylation in human K562 cells after 6 hrs by phospho-flow cytometry 22148584
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50=0.1μM. 22221201
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50=0.5μM. 22221201
K562 Cytotoxicity assay 24 hrs Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50=0.1μM. 22632935
K562 Cytotoxicity assay 48 to 72 hrs Cytotoxicity against human BCR-ABL positive K562 cells after 48 to 72 hrs by MTT assay, IC50=0.3844μM. 22789429
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTS assay, GI50=0.39μM. 22932313
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50=0.11μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50=0.129μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50=0.362μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50=0.424μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50=0.96μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50=1.444μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50=1.834μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50=1.863μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50=2.377μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50=2.547μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50=2.951μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50=3.005μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50=3.763μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50=8.615μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50=17.083μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50=18.52μM. 23088644
MDCK2 Function assay 5 mins Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50=0.04μM. 23241029
HEK293 Function assay 1.5 mins Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50=0.05μM. 23241029
HEK293 Function assay 1.5 mins Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=0.35μM. 23241029
HEK293 Function assay 1.5 mins Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=2.9μM. 23241029
HEK293 Function assay 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=4.2μM. 23241029
HEK293 Function assay 3 mins Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=25.5μM. 23241029
insect cells Function assay 30 mins Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50=0.0982μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.1143μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.115μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.1739μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.24μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.3599μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.4858μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.5μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.59μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.7496μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=1μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=1.6μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=3.3μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=3.6μM. 23301703
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50=5.155μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=5.2μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=5.6μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=9.2μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=9.5μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=11.1μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.2μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.2μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.5μM. 23301703
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=13.5μM. 23301703
BA/F3 Cytotoxicity assay 48 hrs Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay, IC50=0.092μM. 23600806
BA/F3 Cytotoxicity assay 48 hrs Cytotoxicity against mouse BA/F3 cells transfected with Bcr-Abl T315I mutant after 48 hrs by XTT assay, IC50=4.79μM. 23600806
Ba/F3 Function assay 1 hr Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis 23600806
Ba/F3 Function assay 1 hr Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis 23600806
Ba/F3 Function assay 1 hr Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis 23600806
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.47μM. 23735826
GISTT1 Function assay 72 hrs Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay, GI50=0.01μM. 23773153
GIST48B Growth inhibition assay 72 hrs Growth inhibition of human GIST48B cells after 72 hrs by SRB assay, GI50=20μM. 23773153
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.5μM. 23932071
HepG2 Antiproliferative assay 24 to 96 hrs Antiproliferative activity against human HepG2 cells after 24 to 96 hrs by MTS assay, IC50=10μM. 23932071
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by calcein-AM assay, IC50=0.5μM. 23981532
K562 Antiproliferative assay 24 hrs In vitro antiproliferative activity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=13μM. 24681986
BV173 Antiproliferative assay 24 hrs In vitro antiproliferative activity against human BV173 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=20μM. 24681986
CCRF-CEM Antiproliferative assay 24 hrs In vitro antiproliferative activity against human CCRF-CEM cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=45μM. 24681986
HGC27 Cytotoxicity assay 48 hrs Cytotoxicity against HGC27 cells assessed as cell viability after 48 hrs by MTT assay, IC50=3.8μM. 24900584
K562 Antiproliferative assay 48 hrs Antiproliferative activity against Bcr/Abl positive human K562 cells after 48 hrs by MTT method, IC50=4.12μM. 25464886
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs using Calcein AM by fluorescence assay, IC50=0.5μM. 25757603
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.47μM. 25778766
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50=0.28μM. 26195136
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=1.16μM. 26231079
K562 Antiproliferative assay 48 hrs Antiproliferative activity against imatinib-resistant human K562 cells after 48 hrs by MTT assay, IC50=15.7μM. 26231079
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=4.12μM. 26298495
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay, IC50=1.16μM. 26451772
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay, IC50=0.089μM. 26562217
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay, IC50=14.5μM. 26562217
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by trypan blue dye exclusion assay, IC50=0.22μM. 26629859
K562 Apoptosis assay 48 hrs Induction of apoptosis in human K562 cells after 48 hrs by annexinV and propidium iodide staining based flow cytometry, AC50=0.68μM. 26629859
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=0.53μM. 26707846
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method, IC50=0.73μM. 26741853
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.14μM. 26789553
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.16μM. 26789553
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.24μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.38μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.5μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.625μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.659μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.855μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=1.69μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=1.93μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.1μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.169μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=3μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=4.1μM. 26789553
HEL Antiproliferative assay 72 hrs Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=5.3μM. 26789553
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=6.7μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=7.7μM. 26789553
BA/F3 Function assay 72 hrs Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=9.7μM. 26789553
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.51μM. 26814890
K562/G Cytotoxicity assay 72 hrs Cytotoxicity against human K562/G cells assessed as cell viability after 72 hrs by MTT assay, IC50=4.65μM. 26814890
BA/F3 Function assay 48 hrs Inhibition of imatinib-resistant PDGFR D842V mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50=0.642μM. 26844689
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=0.03μM. 26850004
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=0.38μM. 26850004
KG1a Antiproliferative assay 72 hrs Antiproliferative activity against human KG1a cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=16.7μM. 26850004
BAF3 Function assay 72 hrs Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, EC50=0.034μM. 27010810
JURL-MK1 Antiproliferative assay 48 hrs Antiproliferative activity against human JURL-MK1 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.06μM. 27011159
BV173 Antiproliferative assay 48 hrs Antiproliferative activity against human BV173 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.1μM. 27011159
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.2μM. 27011159
EM2 Antiproliferative assay 48 hrs Antiproliferative activity against human EM2 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.26μM. 27011159
KCL22 Antiproliferative assay 48 hrs Antiproliferative activity against human KCL22 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.43μM. 27011159
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.008μM. 27077705
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.014μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.039μM. 27077705
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.074μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.1μM. 27077705
K562 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.12μM. 27077705
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.16μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.4μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=1.29μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=2.49μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=3μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=6.67μM. 27077705
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by XTT assay, IC50=0.31μM. 27214512
A10 Function assay 68 hrs Inhibition of PDGFR-beta driven proliferation of rat A10 cells after 68 hrs in presence of rat recombinant PDGF-BB by cell titer-glo luminescence assay, IC50=0.162μM. 27502700
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT L567P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.01μM. 27545040
GIST-T1 Function assay 72 hrs Inhibition of wild type cKIT in human GIST-T1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.027μM. 27545040
Sf9 Function assay 1 hr Inhibition of His-tagged cKIT (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase assay, IC50=0.319μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.36μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.59μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.7μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.7μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT T670I/V559D double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=5.2μM. 27545040
GIST-5R Function assay 72 hrs Inhibition of wild type cKIT T670I mutant in human GIST-5R cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=8.3μM. 27545040
BA/F3 Function assay 72 hrs Inhibition of TEL-fused cKIT T670I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=9.6μM. 27545040
Sf9 Function assay 1 hr Inhibition of His-tagged cKIT T670I mutant (544 to 935 residues) (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase assay, IC50=9.818μM. 27545040
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.008μM. 27966954
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.014μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.019μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.034μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.039μM. 27966954
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.074μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.102μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.11μM. 27966954
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.163μM. 27966954
SF9 Function assay 1 hr Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay, IC50=0.223μM. 27966954
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.267μM. 27966954
BAF3 Function assay 72 hrs Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.27μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.37μM. 27966954
BAF3 Function assay 72 hrs Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.625μM. 27966954
BAF3 Function assay 72 hrs Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.85μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=1.29μM. 27966954
BAF3 Function assay 72 hrs Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=1.79μM. 27966954
BAF3 Function assay 72 hrs Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=2.16μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=2.49μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=3μM. 27966954
BAF3 Function assay 72 hrs Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=6.67μM. 27966954
K562 Function assay 30 mins Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.043μM. 28280261
K562 Function assay 30 mins Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.09μM. 28280261
K562 Function assay 30 mins Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.25μM. 28280261
K562 Function assay 30 mins Inhibition of kinobead binding to ARG in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.272μM. 28280261
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.53μM. 28525838
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=4.56μM. 28525838
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.003μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0107μM. 28541695
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against human GIST882 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.02μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT C674S mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0249μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT V559D mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.036μM. 28541695
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human MEG01 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.045μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT L576P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0451μM. 28541695
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against human KU812 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.11μM. 28541695
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.147μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT A829P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.1482μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.3819μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.803μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.8031μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT D816H mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=1.245μM. 28541695
BAF3 Function assay 72 hrs Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=1.466μM. 28541695
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=4.686μM. 28541695
GIST48B Antiproliferative assay 72 hrs Antiproliferative activity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=6.986μM. 28541695
BAF3 Function assay 72 hrs Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.73μM. 28974338
BAF3 Function assay 72 hrs Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=20.03μM. 28974338
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50=0.04μM. 28991465
GIST430 Cytotoxicity assay 72 hrs Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50=1.1μM. 28991465
EOL-1 Antiproliferative assay 72 hrs Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50<0.001μM. 29544149
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRbeta (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.019μM. 29544149
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.034μM. 29544149
NCI-H1703 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay, GI50=0.23μM. 29544149
BA/F3 Function assay 72 hrs Inhibition of TEL-fused c-KIT (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.37μM. 29544149
NCI-H1703 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.1μM. 29544149
K562 Cytotoxicity assay 48 hrs Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay, IC50=1.1μM. 29655981
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=3.43μM. 29684708
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=7.12μM. 29684708
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50=8.9μM. 29684708
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=19.66μM. 29684708
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50=0.06μM. 29724653
GIST882 Antiproliferative assay 96 hrs Antiproliferative activity against imatinib-susceptible human GIST882 cells harboring c-KIT K642E mutant after 96 hrs by SRB assay, IC50=1.7μM. 29724653
HGC27 Antiproliferative assay 96 hrs Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50=2.4μM. 29724653
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50=11.3μM. 29724653
GIST48 Antiproliferative assay 96 hrs Antiproliferative activity against imatinib-resistant human GIST48 cells harboring c-KIT V560D/D820A double mutant after 96 hrs by SRB assay, IC50=19.8μM. 29724653
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.0771μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.0905μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.149μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.201μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.249μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.455μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.836μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.838μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.874μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=9.645μM. 30137981
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.017μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.046μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.07μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.102μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.192μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.216μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.223μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.312μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.392μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.535μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.567μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.669μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.701μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=1.191μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=1.523μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=2.749μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=3.947μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=9.93μM. 30204441
K562 Cytotoxicity assay 24 hrs Cytotoxicity against imatinib-sensitive human K562 cells assessed as decrease in cell viability after 24 hrs by XTT assay, IC50=1μM. 30261468
Sf9 Function assay 60 mins Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G, IC50=0.043μM. 30317026
K562 Antiproliferative assay 72 hrs Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay, GI50=0.25μM. 30317026
BAF3 Function assay 72 hrs Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.26μM. 30317026
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay, GI50=0.28μM. 30317026
BAF3 Function assay 72 hrs Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.29μM. 30317026
KU812 Antiproliferative assay 72 hrs Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay, GI50=0.31μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.65μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.85μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.95μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.17μM. 30317026
Sf9 Function assay 1 hr Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay, IC50=1.5μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=2.24μM. 30317026
BAF3 Function assay 72 hrs Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=3.75μM. 30317026
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay, IC50=44.55μM. 30562697
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=0.00015μM. 30605831
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.33μM. 30798049
MDA-MB-453 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=12.84μM. 30798049
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.001μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.005μM. 31046271
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant incubated for 72 hrs by CCK8 assay, GI50=0.026μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.039μM. 31046271
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against human GIST882 cells harboring c-KIT K642E mutant incubated for 72 hrs by CCK8 assay, GI50=0.058μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.115μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.267μM. 31046271
BAF3 Function assay 72 hrs Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.364μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.406μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.823μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.29μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.57μM. 31046271
BAF3 Function assay 72 hrs Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=2.3μM. 31046271
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by real time live-cell imaging technique, IC50=0.14μM. 31097376
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human BCR/ABL positive K562 cells assessed as growth inhibition measured after 48 hrs by MTT assay, IC50=4.26μM. 31185413
BAF3 Function assay 72 hrs Inhibition of c-KIT V560D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.003μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT V559G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.008μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT V559D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.01μM. 31250638
GISTT1 Function assay 72 hrs Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.015μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT D820E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.035μM. 31250638
GIST882 Function assay 72 hrs Inhibition of c-KIT K642E mutant in human GIST882 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.048μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT L576P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.085μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT S709F mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.115μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT D816E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.174μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT D820G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.337μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.35μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT D820Y mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.435μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT A829P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.58μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT V654A/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.608μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT D816H mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.651μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT V559A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.905μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT V654A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.41μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT N822K mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.47μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT T670E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=4.08μM. 31250638
BAF3 Function assay 72 hrs Inhibition of c-KIT Y823D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=5.87μM. 31250638
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant measured after 72 hrs by CCK8 assay 31250638
EOL-1 Cytotoxicity assay 72 hrs Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50<0.0005μM. 31514019
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50=0.73μM. 31514019
CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50=35.809μM. 31514019
Ba/F3 Function assay 72 hrs Inhibition of wild type BCR/Abl (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.1438μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl P230 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.2215μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl P190 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.3455μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl F317I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.364μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl V299L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.4053μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl Q252H mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.4865μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl F317L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.7163μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl M351T mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.7993μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl H396P mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=2.706μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl E255K mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=3.257μM. 31699612
Ba/F3 Function assay 72 hrs Inhibition of BCR/Abl Y253F mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=8.778μM. 31699612
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay, GI50=0.04μM. 31721578
Sf9 Function assay 150 mins Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of , IC50=0.053μM. 31721578
Sf9 Function assay 4 hrs Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine, IC50=0.131μM. 31721578
GIST882 Antiproliferative assay 144 hrs Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay, GI50=0.195μM. 31721578
GIST430 Antiproliferative assay 120 hrs Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining , GI50=0.625μM. 31721578
GIST48 Antiproliferative assay 120 hrs Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay, GI50=0.929μM. 31721578
CTV-1 Growth Inhibition Assay IC50=33.9789 μM SANGER
Calu-6 Growth Inhibition Assay IC50=33.1855 μM SANGER
EW-1 Growth Inhibition Assay IC50=32.9454 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=30.5093 μM SANGER
ES1 Growth Inhibition Assay IC50=27.521 μM SANGER
L-540 Growth Inhibition Assay IC50=26.9143 μM SANGER
LS-513 Growth Inhibition Assay IC50=26.8847 μM SANGER
NB10 Growth Inhibition Assay IC50=26.4699 μM SANGER
MPP-89 Growth Inhibition Assay IC50=25.6874 μM SANGER
DMS-79 Growth Inhibition Assay IC50=24.4934 μM SANGER
GDM-1 Growth Inhibition Assay IC50=22.5945 μM SANGER
ALL-PO Growth Inhibition Assay IC50=20.8149 μM SANGER
RS4-11 Growth Inhibition Assay IC50=20.3308 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=20.1246 μM SANGER
NKM-1 Growth Inhibition Assay IC50=19.3552 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=18.4452 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=18.1848 μM SANGER
LC4-1 Growth Inhibition Assay IC50=18.0652 μM SANGER
HH Growth Inhibition Assay IC50=17.3999 μM SANGER
TE-441-T Growth Inhibition Assay IC50=17.2886 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=17.2442 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=16.6094 μM SANGER
ES7 Growth Inhibition Assay IC50=14.7379 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=14.3335 μM SANGER
SCC-15 Growth Inhibition Assay IC50=10.7788 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=8.34052 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=8.07384 μM SANGER
IMR-5 Growth Inhibition Assay IC50=6.22147 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=5.57262 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=3.82907 μM SANGER
BE-13 Growth Inhibition Assay IC50=2.62106 μM SANGER
A498 Growth Inhibition Assay IC50=2.57223 μM SANGER
NOS-1 Growth Inhibition Assay IC50=1.65383 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=0.97801 μM SANGER
ST486 Growth Inhibition Assay IC50=0.6854 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.38374 μM SANGER
K-562 Growth Inhibition Assay IC50=0.22432 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.1874 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.08921 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.0888 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.07304 μM SANGER
YT Growth Inhibition Assay IC50=38.5209 μM SANGER
TE-6 Growth Inhibition Assay IC50=41.2798 μM SANGER
HT-144 Growth Inhibition Assay IC50=41.5486 μM SANGER
EW-13 Growth Inhibition Assay IC50=42.2791 μM SANGER
KALS-1 Growth Inhibition Assay IC50=43.1329 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=45.0752 μM SANGER
D-336MG Growth Inhibition Assay IC50=45.9599 μM SANGER
TE-11 Growth Inhibition Assay IC50=46.653 μM SANGER
EB2 Growth Inhibition Assay IC50=46.699 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=48.0961 μM SANGER
SW684 Growth Inhibition Assay IC50=48.2695 μM SANGER
EW-18 Growth Inhibition Assay IC50=48.4395 μM SANGER
RL95-2 Growth Inhibition Assay IC50=50.071 μM SANGER
CHP-126 Growth Inhibition Assay IC50=50.8905 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=51.7835 μM SANGER
TE-15 Growth Inhibition Assay IC50=52.2556 μM SANGER
ES4 Growth Inhibition Assay IC50=52.9775 μM SANGER
TE-1 Growth Inhibition Assay IC50=53.9455 μM SANGER
SIMA Growth Inhibition Assay IC50=57.3311 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=64.1188 μM SANGER
KY821 Growth Inhibition Assay IC50=64.2552 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=65.7601 μM SANGER
KP-N-RT-BM-1 Growth Inhibition Assay IC50=66.6366 μM SANGER
SW872 Growth Inhibition Assay IC50=67.4382 μM SANGER
ES5 Growth Inhibition Assay IC50=67.6968 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=68.3803 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=71.032 μM SANGER
UACC-812 Growth Inhibition Assay IC50=71.1609 μM SANGER
COLO-829 Growth Inhibition Assay IC50=72.6987 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=72.7139 μM SANGER
GI-1 Growth Inhibition Assay IC50=73.2868 μM SANGER
ETK-1 Growth Inhibition Assay IC50=73.4932 μM SANGER
LXF-289 Growth Inhibition Assay IC50=73.729 μM SANGER
CAS-1 Growth Inhibition Assay IC50=73.8857 μM SANGER
EW-22 Growth Inhibition Assay IC50=74.7115 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=75.6379 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=81.6963 μM SANGER
D-247MG Growth Inhibition Assay IC50=82.0248 μM SANGER
Becker Growth Inhibition Assay IC50=82.3481 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=82.3482 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=82.5996 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=84.0197 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=86.1618 μM SANGER
HCC2218 Growth Inhibition Assay IC50=86.7913 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=87.7699 μM SANGER
AM-38 Growth Inhibition Assay IC50=88.3953 μM SANGER
KNS-42 Growth Inhibition Assay IC50=89.1018 μM SANGER
C8166 Growth Inhibition Assay IC50=89.6125 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=89.8719 μM SANGER
CTB-1 Growth Inhibition Assay IC50=90.6357 μM SANGER
HCE-4 Growth Inhibition Assay IC50=91.1336 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=92.4103 μM SANGER
ECC4 Growth Inhibition Assay IC50=94.2555 μM SANGER
NCCIT Growth Inhibition Assay IC50=95.3292 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=95.904 μM SANGER
COLO-684 Growth Inhibition Assay IC50=96.2385 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=96.9842 μM SANGER
SF126 Growth Inhibition Assay IC50=97.5217 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=98.4554 μM SANGER
NB14 Growth Inhibition Assay IC50=98.9208 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=99.4056 μM SANGER
CHO Function assay Inhibition of wild type Platelet-derived growth factor receptor beta phosphorylation in CHO cells, IC50=0.24μM. 12166950
CHO Function assay Inhibition of chimeric PDGF receptor with c-kit cytoplasmic domain phosphorylation in CHO cells, IC50=0.26μM. 12166950
CHO Function assay Inhibition of chimeric PDGF receptor with CSF-1R cytoplasmic domain phosphorylation in CHO cells, IC50=0.96μM. 12166950
K562 Cytotoxicity assay Cytotoxic effect in K562 cells, IC50=0.11μM. 12951113
K562 Function assay Inhibitory activity against human K562 cells growth using MTT assay, IC50=0.4μM. 14552760
Sf9 Function assay TP_TRANSPORTER: inhibition of ATPase activity in BCRP-expressing Sf9 cells, IC50=0.5μM. 15155841
Sf9 Function assay TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells, IC50=0.9μM. 15155841
K562 Antiproliferative assay Antiproliferative activity against K562 cells, IC50=0.182μM. 16332440
U937 Antiproliferative assay Antiproliferative activity against U937 cells, IC50=14μM. 16332440
32D Cytotoxicity assay Cytotoxic activity against mouse 32D cells transfected with p210 Bcr-abl, IC50=0.19μM. 16415863
32D Cytotoxicity assay Cytotoxic activity against mouse 32D Bcr-abl negative cells, IC50=20μM. 16415863
BaF3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50=7.1μM. 16970400
BaF3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50=9.1μM. 16970400
Sf9 Function assay Inhibition of human Lyn kinase expressed in Sf9 cells, IC50=0.22μM. 17376680
Sf9 Function assay Inhibition of human Abl kinase expressed in Sf9 cells, IC50=0.47μM. 17376680
K562 Cytotoxicity assay Cytotoxicity against K562 cells by MTT assay, IC50=0.18μM. 17572088
A2780/ADR Function assay Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50=7.24436μM. 17890094
MO7e Function assay Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay, IC50=0.046μM. 18447379
MCF7 Function assay Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50=4.89779μM. 18678495
A2780 Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=7.24436μM. 18678495
CML Antiproliferative assay Antiproliferative activity against human CML cells, IC50=0.35μM. 19219016
ALL3 Cytotoxicity assay Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay, IC50=0.333μM. 19889540
MDCK Function assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=3.38μM. 19932960
MCF7 MX Function assay Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=4.07μM. 19932960
BA/F3 Antiproliferative assay Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50=0.039μM. 20817538
HEK293 Function assay Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50=0.043μM. 20817538
A31 Function assay Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50=0.072μM. 20817538
A31 Function assay Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50=0.072μM. 20817538
GIST882 Function assay Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50=0.097μM. 20817538
GIST882 Antiproliferative assay Antiproliferative activity against human GIST882 cells, IC50=0.108μM. 20817538
HEK293 Function assay Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50=0.141μM. 20817538
Ba/F Function assay Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50=0.221μM. 20817538
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50=0.244μM. 20817538
HEK293 Function assay Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50=0.291μM. 20817538
M-NFS-60 Antiproliferative assay Antiproliferative activity against mouse M-NFS-60 cells, IC50=0.358μM. 20817538
K562 Function assay Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50=0.473μM. 20817538
BA/F3 Antiproliferative assay Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50=0.678μM. 20817538
BA/F3 Antiproliferative assay Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3, IC50=9.459μM. 20817538
K562 Antiproliferative assay Antiproliferative activity against human imatinib-resistant K562 cells, IC50=0.00605μM. 21376587
KU812 Antiproliferative assay Antiproliferative activity against human KU812 cells, IC50=0.337μM. 21376587
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50=0.38μM. 21376587
Sf9 Function assay Binding affinity to human active site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd=0.006μM. 21417343
Sf9 Function assay Binding affinity to human remote site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd=0.5μM. 21417343
TF1 Cytotoxicity assay Cytotoxicity against human TF1 cells expressing c-KIT mutation assessed as cell viability, IC50=0.013μM. 22221201
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, GI50=0.17μM. 22439674
HUVEC Antiproliferative assay Antiproliferative activity against HUVEC cells, GI50=18.5μM. 22439674
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50=0.5μM. 23352483
K562 Cytotoxicity assay Cytotoxicity against human K562 cells, IC50=0.17μM. 23600806
GIST882 Function assay Inhibition of KIT K642E mutant autophosphorylation (unknown origin) expressed in human GIST882 cells by ELISA, IC50=0.097μM. 23611771
GIST882 Function assay Inhibition of KIT K642E mutant (unknown origin) expressed in human GIST882 cells assessed as cell growth inhibition by ATP-depletion assay, IC50=0.108μM. 23611771
32D Function assay Inhibition of human BCR-ABL1 (unknown origin) expressed in mouse 32D cells, IC50=0.194μM. 23611771
BA/F3 Function assay Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA, IC50=0.221μM. 23611771
BA/F3 Function assay Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay, IC50=0.678μM. 23611771
Sf9 Function assay Inhibition of recombinant Abl kinase (unknown origin) expressed in Sf9 cells using GGEAIYAAPFKK as substrate in presence of [gamma33P]ATP, IC50=0.3μM. 24681986
HMC-1.2 Antiproliferative assay Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay, IC50=17μM. 25004409
K562 Cytotoxicity assay Cytotoxicity against human K562 cells assessed as reduction in cell viability, IC50=0.06μM. 26264503
IR-K562 Cytotoxicity assay Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability, IC50=1.1μM. 26264503
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability, CC50=8.4μM. 26264503
U937 Cytotoxicity assay Cytotoxicity against human U937 cells assessed as reduction in cell viability, IC50=19μM. 26264503
THP1 Cytotoxicity assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability, IC50=25μM. 26264503
HCT116 Anticancer assay Anticancer activity against human HCT116 cells, IC50=34.4μM. 26312434
293T Cytotoxicity assay Cytotoxicity against human 293T cells assessed as growth inhibition, CC50=20.53μM. 26850004
K562 Cytotoxicity assay Cytotoxicity against human K562 cells, IC50=0.5μM. 27189674
Sf9 Function assay Binding affinity to recombinant full length human N-terminal GST-tagged Syk-KD (356 to 635 residues) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells using poly EY 4:1 as substrate, Ki=5μM. 29132752
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
GIST882 Antiproliferative assay Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay, GI50=0.195μM. 30968693
GIST882 Antiproliferative assay Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.195μM. 30968693
GIST48 Antiproliferative assay Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay, GI50=0.625μM. 30968693
GIST48 Antiproliferative assay Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.625μM. 30968693
Sf9 Function assay Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation, IC50=0.769μM. 30968693
GIST430 Antiproliferative assay Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay, GI50=0.929μM. 30968693
GIST430 Antiproliferative assay Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.929μM. 30968693
Sf9 Function assay Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation, IC50=5.21μM. 30968693
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生物活性

产品描述 Imatinib是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。
特性 Imatinib 是多靶点酪氨酸激酶抑制剂。
靶点
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
体外研究(In Vitro)
体外研究活性

体外抑制一组酪氨酸和丝/苏氨酸蛋白激酶实验,说明Imatinib有效抑制v-Abl 酪氨酸激酶和PDGFR,IC50 分别为 0.6 和 0.1 μM。[1]

Imatinib抑制 野生型 c-kit激酶活性的SLF依赖性激活,IC50约为0.1 μM, 与抑制PDGFR所需的浓度相似。[2]

Imatinib 抑制人类支气管类癌细胞NCI-H727和胰腺类癌细胞 BON-1生长,IC50分别为 32.4 和 32.8 μM。[3]

最新研究显示Imatinib作用于慢性粒细胞白血病,通过下调hERG1 K(+)通道,具有恢复其抗白血病效果的潜力,而hERG1 K(+) 通道在白血病细胞中高表达,且易引发白血病。[4]

激酶实验 PDGF 受体激酶活性
从BALB/c 3T3 细胞抽提物中使用兔抗血清免疫沉淀PDGF受体,然后小鼠PDGF受体置于冰上2小时。使用蛋白A-琼脂糖磁珠,用于收集抗原-抗体复合体。使用TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100)冲洗免疫沉淀反应两次,,使用TNE (50 mM Tris, pH 7.5, 140 mM EDTA)冲洗一次,再使用激酶 buffer (20 mM Tris, pH 7.5,10 mM MgCl2)冲洗一次。在 4oC下使用PDGF(50 ng/mL)刺激10分钟,在反应混合物中加入不同浓度Imatinib。与10 μCi [7-33P]-ATP及l μM ATP 在4oC下温育10分钟,然后测定PDGF受体激酶活性。通过 SDS-PAGE 在7.5% 凝胶上分离免疫复合物。
细胞实验 细胞系 BON-1 和 NCI-H727 细胞
浓度 0 到 100 μM
孵育时间 48 小时
方法

BON-1 细胞和 NCI-H727 细胞按一式三份接种在平底96孔板上,分别在补充10%胎牛血清的 DMEM 或 RPMI 1640 完全培养基中粘附过夜,更换培养基为无血清培养基(阴性对照) 或含连续稀释Imatinib的无血清培养基。48小时后 (对照组细胞不汇合),通过MTT实验测定代谢活性细胞数,使用Packard Spectra 酶标仪在540 nm处测定吸光值。按如下公式计算抑制生长率: 抑制率=(1 − a / b) × 100%, a 和 b 分别为实验组和对照组的吸光值。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-STAT3 / STAT3 / p-STAT5 / STAT5 p-ZAP70 / ZAP70 / p-LAT / LAT p-STAT3 / STAT3 / p-STAT5 / STAT5 p-ZAP70 / ZAP70 / p-LAT / LAT 18981115
Immunofluorescence RelB Cortactin / F-actin RelB Cortactin / F-actin 20371728
Growth inhibition assay Cell viability 28435223
体内研究(In Vivo)
体内研究活性

Imatinib作用于三种从新鲜人类小细胞肺癌衍生的移植瘤,具有不同的抗肿瘤效果,抑制SCLC6, SCLC61和 SCLC108 肿瘤生长分别达80%, 40% 和78%,而对SCLC74 生长没有明显抑制效果。[5]

Imatinib 处理高脂肪饲喂的ApoE(-/-)小鼠, 显著降低高脂肪诱导的脂质染色区,按10,20和 40 mg/kg剂量饲喂,与未经高脂肪饮食处理的对照组相比,脂质染色区分别降低 30%, 27% 和 35%,且抑制颈动脉脂质堆积。[6]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05493215 Recruiting
Gastrointestinal Stromal Tumors
Reema A. Patel|University of Kentucky
March 26 2024 Phase 2
NCT06090669 Recruiting
Inherited Bone Marrow Failure Syndrome|Familial Platelet Disorder With Predisposition to Myeloid Malignancies
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
December 19 2023 Phase 1
NCT05413915 Recruiting
Chronic Myeloid Leukemia|Chronic Myeloid Leukemia BCR/ABL-Positive|Chronic Myeloid Leukemia in Remission
Sarit Assouline|Novartis|Sir Mortimer B. Davis - Jewish General Hospital
June 19 2023 Phase 3
NCT05816785 Recruiting
Head and Neck Cancer|Squamous Cell Carcinoma of Head and Neck
University of Wisconsin Madison|National Cancer Institute (NCI)
April 18 2023 Early Phase 1
NCT05623774 Recruiting
CML
Inhibikase Therapeutics Inc.
December 16 2022 Phase 1
NCT05282108 Recruiting
Chronic Myeloid Leukemia
Hikma Pharmaceuticals LLC
July 20 2022 --

化学信息&溶解度

分子量 493.6 分子式

C29H31N7O

CAS号 152459-95-5 SDF Download Imatinib SDF
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 25 mg/mL ( (50.64 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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常见问题及建议解决方法

问题 1:
Could you please advise whether it is a clear solution for compound dissolved in vehicle 2% DMSO+30% PEG 300+2% Tween 80+ddH2O?

回答:
For S2475 Imatinib (STI571), it is soluble in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 2mg/ml. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm it in water bath at 45-50C. Then add PEG and Tween. After they mixed well, dilute with water.

问题 2:
What is the difference between S2475 (Imatinib) and S1026 (Imatinib Mesylate)? Are they water soluble?

回答:
S2475 is free base of Imatinib while S1026 is a solt form of Imatinib. They have exactly the same biological activity but different solubility. S1026 can be dissolved in water, but S2475 is not soluble in water. S2475 can be dissolved in DMSO at up to 3mg/ml.

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