Foretinib

别名: GSK1363089, EXEL-2880, XL-880, GSK089

Foretinib是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。

Foretinib Chemical Structure

Foretinib Chemical Structure

CAS: 849217-64-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2340.27 现货
5mg RMB 1374.78 现货
50mg RMB 7124.95 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

客户使用Selleck的Foretinib发表文献93

产品质控

批次: S111106 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 纯度: 99.82%
99.82

Foretinib相关产品

相关信号通路图

c-Met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
U251 Function Assay 100/300/900 nM 24 h abrogates migration and invasion of glioma cells in a dose dependent manner 24658326
SF188 Function Assay 100/300/900 nM 24 h abrogates migration and invasion of glioma cells in a dose dependent manner 24658326
A172 Growth Inhibition Assay 100/300/900 nM 48 h reduces cell survival at 900 nM significantly 24658326
U251 Growth Inhibition Assay 100/300/900 nM 48 h reduces cell survival at 900 nM significantly 24658326
SF188 Growth Inhibition Assay 100/300/900 nM 48 h reduces cell survival at 900 nM significantly 24658326
SF188 Function Assay 100/300/900 nM 28 h induces PARP cleavage 24658326
U251 Function Assay 100/300/900 nM 28 h induces PARP cleavage 24658326
SF188 Function Assay 100/300/900 nM 1 h decreases Akt phosphorylation in a concentration dependent manner 24658326
A172 Function Assay 100/300/900 nM 1 h decreases Akt phosphorylation in a concentration dependent manner 24658326
U251 Function Assay 100/300/900 nM 1 h decreases Akt phosphorylation in a concentration dependent manner 24658326
SF188 Function Assay 100/300/900 nM 1 h inhibits the activity of Axl, Tyro3 24658326
A172 Function Assay 100/300/900 nM 1 h inhibits the activity of Axl, Tyro3 24658326
U251 Function Assay 100/300/900 nM 1 h inhibits the activity of Axl, Tyro3 24658326
SF188 Function Assay 100/300/900 nM 1 h inhibits the phosphorylation of MerTK  24658326
A172 Function Assay 100/300/900 nM 1 h inhibits the phosphorylation of MerTK  24658326
U251 Function Assay 100/300/900 nM 1 h inhibits the phosphorylation of MerTK  24658326
Daoy  Growth Inhibition Assay 0.5/1/2.5 μM 24-96 h inhibits cell growth in a dose dependent manner 25391241
Daoy  Apoptosis Assay 1 μM 24 h induces apoptosis 25391241
ONS76 Function Assay 0.5/1/2.5 μM 24 h inhibits HGF-mediated migration and invasion 25391241
Daoy  Function Assay 0.5/1/2.5 μM 24 h inhibits HGF-mediated migration and invasion 25391241
ONS76 Function Assay 0.5/1/2.5 μM 24 h inhibits the HGF-induced cMET pathway activation 25391241
Daoy  Function Assay 0.5/1/2.5 μM 24 h inhibits the HGF-induced cMET pathway activation 25391241
A172 Function Assay 100/300/900 nM 24 h abrogates migration and invasion of glioma cells in a dose dependent manner 24658326
Ba/F3 Cell Viability Assay 0.0001-10 μM 72 h inhibits cell growth in a dose dependent manner 24218589
HCC78 Cell Viability Assay 0.01-10 μM 72 h inhibits cell growth in a dose dependent manner 24218589
SK-HEP1 Cell Viability Assay 0.25-1.5 μM 24 h inhibits cell growth in a dose dependent manner 22187171
SK-HEP2 Function Assay 1 μM 24 h blocks HGF-induced cell motility 22187171
SK-HEP2 Function Assay 1 μM 24 h causes G2/M phase arrest with reduction in the G0/G1 and S phases 22187171
MKN-45  Growth Inhibition Assay 0.01-10 μM 5 d IC50=8 nM 21655918
KATO-III Growth Inhibition Assay 0.01-10 μM 5 d IC50=30 nM 21655918
MKN-45  Function Assay 1 μM 24 h inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45 21655918
KATO-III Function Assay 1 μM 24 h inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45 21655918
HCC827 Apoptosis assay 0.01 to 1 uM 72 hrs Induction of apoptosis in gefitinib resistant human HCC827 cells at 0.01 to 1 uM after 72 hrs by annexin V-FITC-propidium iodide staining-based flow cytometry method relative to control 28787156
HCC827 Function assay 0.1 to 0.5 uM 72 hrs Inhibition of MET phosphorylation at Tyr1234/1235 in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method 28787156
HCC827 Function assay 0.1 to 0.5 uM 72 hrs Downregulation of SMO expression in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method 28787156
HCC827 Function assay 0.1 to 0.5 uM 72 hrs Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in MAPK44/42 phosphorylation at Thr202/Tyr204 at 0.1 to 0.5 uM after 72 hrs by Western blotting method 28787156
HCC827 Function assay 0.1 to 0.5 uM 72 hrs Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in AKT phosphorylation at Ser473 at 0.1 to 0.5 uM after 72 hrs by Western blotting method 28787156
HCC827 Function assay 0.1 to 0.5 uM 72 hrs Inhibition of MET/SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in vimentin expression at 0.1 to 0.5 uM after 72 hrs by Western blotting method 28787156
NCI-H1993 Function assay 1 uM 4 hrs Inhibition of c-MET D1228V mutant in CRISPR/Cas9 modified human NCI-H1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis 31531204
NCI-H1993 Function assay 1 uM 4 hrs Inhibition of c-Met phosphorylation in human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis 31531204
NCI-1993 Function assay 1 uM 4 hrs Inhibition of c-MET in human NCI-1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis 31531204
NCI-H1993 Function assay 1 uM 4 hrs Inhibition of c-Met D1228V mutant phosphorylation in CRISPR/Cas9 modified human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis 31531204
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay, IC50 = 0.5 μM. 28787156
HCC827 Antitumor assay 15 mg/kg Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 15 mg/kg/day, po 28787156
HCC827 Antitumor assay 20 mg/kg Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po 28787156
HCC827 Antitumor assay 20 mg/kg Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of gefitinib 28787156
HCC827 Antitumor assay 20 mg/kg Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of osimertinib 28787156
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-dependent human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.03 μM. 23628470
A549 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-dependent human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.08 μM. 23628470
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-dependent human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.15 μM. 23628470
H460 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-independent human H460 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.18 μM. 23628470
SMMC7721 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-dependent human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.44 μM. 23628470
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against c-Met-dependent human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.9 μM. 23628470
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.031 μM. 23644189
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.12 μM. 23644189
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.18 μM. 23644189
SMMC7721 Cytotoxicity assay 72 hrs Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.3 μM. 23644189
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.04 μM. 23644189
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM. 23838381
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.029 μM. 23838381
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.165 μM. 23838381
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM. 23838381
NCI-H460 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM. 23838381
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM. 23838381
SMMC7721 Cytotoxicity assay 72 hrs Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.32 μM. 23838381
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.47 μM. 23838381
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM. 24012712
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.11 μM. 24012712
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM. 24012712
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM. 24012712
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.08 μM. 24012712
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM. 24485123
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM. 24485123
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM. 24485123
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM. 24485123
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.1 μM. 24485123
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM. 24882675
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM. 24882675
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM. 24882675
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM. 24882675
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM. 24996144
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.11 μM. 24996144
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM. 24996144
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM. 24996144
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.08 μM. 24996144
MKN45 Antiproliferative assay 72 hrs Antiproliferative activity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM. 25282672
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.12 μM. 25282672
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM. 25282672
H460 Antiproliferative assay 72 hrs Antiproliferative activity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM. 25282672
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.02 μM. 25282672
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM. 25438768
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM. 25438768
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM. 25438768
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM. 25438768
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.92 μM. 25438768
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.032 μM. 26169763
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.12 μM. 26169763
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.19 μM. 26169763
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.21 μM. 26169763
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM. 26810712
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM. 26810712
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM. 26810712
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM. 26897090
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM. 26897090
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM. 26897090
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.26 μM. 26923692
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.49 μM. 26923692
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM. 26923692
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 6.25 μM. 26923692
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM. 26944614
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.13 μM. 26944614
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.16 μM. 26944614
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM. 26944614
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 1.1 μM. 26944614
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM. 26964675
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM. 26964675
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM. 26964675
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0092 μM. 27068889
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells measured after 72 hrs by MTT assay, IC50 = 0.032 μM. 27155466
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay, IC50 = 0.11 μM. 27155466
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells measured after 72 hrs by MTT assay, IC50 = 0.19 μM. 27155466
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells measured after 72 hrs by MTT assay, IC50 = 0.21 μM. 27155466
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM. 27187857
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.17 μM. 27187857
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.26 μM. 27187857
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM. 27187857
Sf9 Function assay 60 mins Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-c, IC50 = 0.0004 μM. 27299736
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met over-expressed human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM. 27490023
A549 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met over-expressed human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.14 μM. 27490023
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met over-expressed human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM. 27490023
H460 Cytotoxicity assay 72 hrs Cytotoxicity against c-Met over-expressed human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.21 μM. 27490023
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM. 28011202
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM. 28011202
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.32 μM. 28011202
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM. 28384549
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.29 μM. 28384549
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.36 μM. 28384549
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM. 28384549
MKN45 Antiproliferative assay 72 hrs Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.03 μM. 28716639
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM. 28716639
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.21 μM. 28716639
H460 Antiproliferative assay 72 hrs Antiproliferative activity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.22 μM. 28716639
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM. 28716639
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.48 μM. 29107421
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.74 μM. 29107421
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.88 μM. 29107421
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 3.92 μM. 29107421
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM. 29197731
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.28 μM. 29197731
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM. 29197731
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.91 μM. 29197731
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.27 μM. 29203143
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.76 μM. 29203143
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 3.13 μM. 29203143
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM. 29331754
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM. 29331754
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM. 29331754
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM. 30216852
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.48 μM. 30216852
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.76 μM. 30216852
MKN45 Antiproliferative assay 72 hrs Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0023 μM. 30248654
EBC1 Antiproliferative assay 72 hrs Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM. 30248654
SNU5 Antiproliferative assay 72 hrs Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0089 μM. 30248654
BAF3 Function assay 72 hrs Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.0092 μM. 30248654
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0396 μM. 30248654
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity in human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.041 μM. 31079967
NCI-H460 Cytotoxicity assay 72 hrs Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.18 μM. 31079967
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.22 μM. 31079967
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.52 μM. 31079967
sf21 Function assay 60 mins Inhibition of wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM. 31531204
sf21 Function assay 60 mins Inhibition of N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM. 31531204
NCI-H1993 Growth inhibition assay 3 days Growth inhibition of CRISPR/Cas9 modified human NCI-H1993 cells harboring cMET D1228V mutant incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.05248 μM. 31531204
NCI-H1993 Growth inhibition assay 3 days Growth inhibition of wild type human NCI-H1993 cells incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.06166 μM. 31531204
NCI-H1993 Function assay 4 hrs Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM. 31531204
NCI-H1993 Function assay 4 hrs Inhibition of c-MET D1228V mutant phosphorylation at Tyr1234/Tyr1235 residues in CRISPR/Cas9 modified human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM. 31531204
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM. 31546197
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM. 31546197
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM. 31546197
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.2 μM. 31629631
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.14 μM. 31629631
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.49 μM. 31629631
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.76 μM. 31629631
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 2.17 μM. 31629631
H1648 Growth Inhibition Assay IC50=1.28 ±0.12 μM 21252284
H1573 Growth Inhibition Assay IC50=1.62 ± 0.05 μM 21252284
H596 Growth Inhibition Assay IC50=1.21 ± 0.17 μM 21252284
HOP92 Growth Inhibition Assay IC50=0.81 ± 0.29 μM 21252284
H69 Growth Inhibition Assay IC50=1.18 ± 0.08 μM 21252284
H1975 Growth Inhibition Assay IC50=1.39 ± 0.33 μM 21252284
SCC15 Growth Inhibition Assay IC50=0.63 ± 0.04 μM 21252284
HN5 Growth Inhibition Assay IC50=0.65 ± 0.26 μM 21252284
MKN45 Cytotoxicity assay Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM. 23838381
BA/F3 Function assay Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells, IC50 = 0.01 μM. 25461320
BT474 Function assay Inhibition of AXL in lapatinib-sensitive human BT474 cells, IC50 = 0.1 μM. 26555154
MKN45 Cytotoxicity assay Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM. 27187857
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells, IC50 = 0.029 μM. 27187857
A549 Cytotoxicity assay Cytotoxicity against human A549 cells, IC50 = 0.165 μM. 27187857
HCC827 Function assay Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting, Ki = 0.0668 μM. 28787156
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
sf21 Function assay Binding affinity to wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis 31531204
sf21 Function assay Binding affinity to N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis 31531204
点击查看更多细胞系数据

生物活性

产品描述 Foretinib是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。
靶点
Met [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
Tie-2 [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
点击更多
0.4 nM 0.86 nM 1.1 nM 2.8 nM 3 nM
体外研究(In Vitro)
体外研究活性 XL880抑制HGF受体家族酪氨酸激酶,对Met和Ron 的IC50 值分别为0.4 nM和3 nM。XL880也会抑制KDR,Flt-1,和Flt-4,IC50值分别为0.9 nM,6.8 nM和2.8 nM。XL880抑制B16F10,A549 和HT29细胞集落生长,IC50分别为40 nM,29 nM和165 nM。[1]一项最近的研究表明,XL880差异性影响胃癌细胞系MKN-45和KATO-III的细胞生长。XL880抑制MKN-45细胞中MET和下游信号分子的磷酸化,而在KATO-III细胞中靶向作用于GFGR2。[2]
激酶实验 激酶抑制试验
激酶抑制使用三种测定形式中的一种进行研究:[33P]磷酰基转移法,荧光素酶耦合的化学发光法,或AlphaScreen酪氨酸激酶技术。IC50s使用XLFit通过非线性回归分析计算。33P-磷酰基转移激酶实验反应在384孔白色,透明底,高结合力微量滴定板(Greiner,Monroe,NC)中进行。板用50 μL体积的涂层缓冲液中的2 μg/well蛋白质或多肽底物涂覆,涂层缓冲液包含40 μg/mL底物(poly(Glu, Tyr) 4:1,22.5 mM Na2CO3,27.5 mM NaHCO3,50 mM NaCl 和3 mM NaN 3。涂层的板用50 μL实验缓冲液洗涤一次,然后在室温下(RT)过夜培养。测试化合物和酶与33P-γ-ATP (3.3 μCi/nmol)结合,总体积为20 μL。反应混合物在室温下培养2小时,然后通过抽吸终止。随后微量滴定板用0.05% Tween-PBS缓冲液(PBST)清洗6次。加入闪烁液(50 μL/well),整合的33P使用MicroBeta闪烁计数器通过液体闪烁光谱法测量。荧光素酶耦合的化学发光反应在384孔白色,含培养基的微量滴定板(Greiner)中进行。第一步,酶和化合物结合,并培养60分钟;加入终体积为20 μL的ATP与多肽底物(poly(Glu, Tyr) 4:1)起始反应,在室温下培养2-4小时。接下来进行激酶反应,加入20 μL等分激酶Glo (Promega,Madison,WI),荧光信号使用Victor酶标仪测量。总ATP消耗限制在50%。AlphaScreenTM酪氨酸激酶测定使用链霉亲和素涂覆的供体珠和PY100抗磷酸酪氨酸抗体涂覆的受体珠进行。生物素化的聚(Glu,Tyr) 4:1用作底物。通过加入供体/受体珠,随后形成供体/受体珠复合物产生荧光测量底物磷酸化。激酶与测试化合物结合,并预培养60分钟,随后加入总体积为20 μL 的ATP,和生物素化的聚(Glu, Tyr)在384孔白色,含培养基的微量滴定板(Greiner)中。反应混合物在室温下培养1小时。然后加入包含75 mM Hepes,pH 7.4,300 mM NaCl,120 mM EDTA,0.3% BSA和0.03% Tween-20的10 μL 15-30 μg/mL AlphaScreen 珠悬浮液淬灭反应。室温下培养2-16小时后,板使用AlphaQuest阅读器读取数据。
细胞实验 细胞系 B16F10,A549,和 HT29 细胞
浓度 40 nM
孵育时间 12 到 14 天
方法 B16F10,A549,和HT29细胞(1.2×103/孔)与软琼脂混合,并接种于包含超过琼脂层的10% FBS 和EXEL-2880的96孔板。对于含氧量正常的条件,板在21%氧气,5% CO2,和74% 氮气中培养(37 ℃)12到14天,而低氧条件下的培养(37℃)在1% 氧气,5% CO2,和94%氮气的低氧培养室中进行。每个条件下的集落数量在加入50% Alamar Blue,进行荧光检测后评估。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-Met / Met / p-Akt / Akt p-MDM2 / p53 / PUMA pROS1 / tROS1 / pSHP2 / pERK / ERK 29854314
Growth inhibition assay Cell viability 29854314
体内研究(In Vivo)
体内研究活性 XL880(100 mg/kg,单一剂量,口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如,HGFor VEGF)诱导的肝脏中Met和肺中Flk-1/KDR受体磷酸化,两者都能持续24小时。XL880 (30-100 mg/kg,每天一次,口服强喂)处理导致肿瘤负荷减少。30和100 mg/kg XL880处理后,肺表面肿瘤负荷分别减少50%和58%。XL880处理负荷B16F10实体瘤的小鼠也会导致剂量依赖性肿瘤生长抑制,30和100 mg/kg分别导致64%和87%的抑制。对于这两项研究,XL880给药具有良好的耐受性,并且没有显著的体重损失。[1] XL880通过Met可以进一步以HGF的反常信号为作用靶点,同时靶向作用于几个参与肿瘤血管生成的受体酪氨酸激酶。XL880给药2到4小时后,引起人异种移植物中肿瘤出血坏死,96小时(给药5天后)观察到最大肿瘤坏死,导致完全的肿瘤消退。[3]
动物实验 Animal Models B16F10 肿瘤细胞(2×10 5)通过胃部静脉注射植入5到8周大的无胸腺裸鼠(NCr 或 BALB/c)
Dosages 100 mg/kg
Administration 口服强饲
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00920192 Completed
Carcinoma Hepatocellular
GlaxoSmithKline
August 12 2009 Phase 1
NCT00742261 Completed
Solid Tumours
GlaxoSmithKline
August 11 2008 Phase 1
NCT00725764 Completed
Neoplasms Head and Neck
GlaxoSmithKline
August 27 2007 Phase 2
NCT00725712 Completed
Neoplasms Gastrointestinal Tract
GlaxoSmithKline
March 31 2007 Phase 2
NCT00743067 Completed
Solid Tumours
GlaxoSmithKline
August 9 2006 Phase 1

化学信息&溶解度

分子量 632.65 分子式

C34H34F2N4O6

CAS号 849217-64-7 SDF Download Foretinib SDF
Smiles COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 158.06 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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