Irinotecan HCl Trihydrate

别名: CPT-11 HCl Trihydrate 中文名称:盐酸依立替康三水合物

Irinotecan HCl Trihydrate是伊立替康的盐酸盐三水合物,伊立替康是一种拓扑异构酶 I 抑制剂,对 LoVo 细胞和 HT-29 细胞的 IC50 分别为 15.8 和 5.17 μM。

Irinotecan HCl Trihydrate Chemical Structure

Irinotecan HCl Trihydrate Chemical Structure

CAS: 136572-09-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1545.43 现货
5mg RMB 571.52 现货
25mg RMB 1722.94 现货
100mg RMB 4332.51 现货
1g RMB 7944.3 现货
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批次: 纯度: 99.97%
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Irinotecan HCl Trihydrate相关产品

相关信号通路图

Topoisomerase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
HEK293 Inhibition of human up to 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 = 7.9 μM. 23241029
MM487 Antiproliferative assay 10 uM 72 hrs Antiproliferative activity against human MM487 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 9.4 μM. 29150335
MM432 Antiproliferative assay 10 uM 72 hrs Antiproliferative activity against human MM432 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 10 μM. 29150335
HT-29 Antitumor assay 60 mg/kg 2 days Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as tumor growth inhibition at 60 mg/kg, iv tid administered 2 days measured on day 20 23360284
BT-483 Function assay 1 uM 24 hrs Induction of DNA damage in human BT-483 cells assessed as gamma H2AX phosphorylation at Ser139 at 1 uM after 24 hrs by Western blot analysis 23419737
HCT116 Antitumor assay 30 mg/kg 6 days Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days 24583355
H3347 Antitumor assay 30 mg/kg 6 days Antitumor activity against human H3347 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days 24583355
SW620 Antitumor assay 12.5 mg/kg Antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 12.5 mg/kg, ip 22111927
HCT116 Antitumor assay 100 mg/kg Antitumor activity against human HCT116 cells xenografted in nu/nu mouse assessed as tumor regression at 100 mg/kg, iv dosed once every week 25003995
NCI-H526 Antitumor assay 30 mg/kg Antitumor activity against human NCI-H526 cells xenografted in athymic nude mouse at 30 mg/kg, iv qd administered 5 times for every 2 days 28064078
A375 Cytotoxicity assay 72 hrs Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM. 21341674
MDA-MB-435 Cytotoxicity assay 3 days Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay, IC50 = 17 μM. 20942490
LoVo Cytotoxicity assay 3 days Cytotoxicity against human LoVo cells after 3 days by MTT assay, IC50 = 8.8 μM. 20942490
A549 Cytotoxicity assay 3 days Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50 = 6.4 μM. 20942490
LoVo Cytotoxicity assay 72 hrs Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50 = 4.99 μM. 20371183
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.61 μM. 20371183
MDA-MB-435 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 1.14 μM. 20371183
LS174T Cytotoxicity assay 96 hrs Cytotoxicity against human LS174T cells after 96 hrs by MTT assay, IC50 = 1.16 μM. 18513976
MCF7 Antitumor assay 4 hrs Antitumor activity against human MCF7 cells after 4 hrs by MTT assay, IC50 = 17.403 μM. 18207748
LOVO Antitumor assay 4 hrs Antitumor activity against human LOVO cells after 4 hrs by MTT assay, IC50 = 9.015 μM. 18207748
A549 Antitumor assay 4 hrs Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50 = 6.528 μM. 18207748
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs, GI50 = 1.9 μM. 25420175
MDA-MB-435 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50 = 12.2 μM. 22867019
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay, GI50 = 7.1 μM. 22867019
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay, GI50 = 5 μM. 22867019
MDA-MB-231 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay, GI50 = 9.17 μM. 22079254
HepG2 Growth inhibition assay 72 hrs Growth inhibition of human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM. 22079254
Hep3B Growth inhibition assay 72 hrs Growth inhibition of human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM. 22079254
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM. 19796956
Hep3B Antiproliferative assay 72 hrs Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM. 19796956
RPMI8402 Cytotoxicity assay 4 days Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment. IC50=0.57 μM 12747798
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM. 21341674
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50 = 0.009 μM. 21341674
MESSA Cytotoxicity assay 72 hrs Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50 = 0.01 μM. 21341674
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay, IC50 = 0.015 μM. 21341674
H69 Cytotoxicity assay 72 hrs Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50 = 0.022 μM. 21341674
MES-SA/Dx5 Cytotoxicity assay 72 hrs Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.022 μM. 21341674
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA, IC50 = 0.027 μM. 21341674
IGROV1 Cytotoxicity assay 72 hrs Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50 = 0.03 μM. 21341674
SK-MEL-2 Cytotoxicity assay 72 hrs Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50 = 0.1 μM. 21341674
MALME-3M Cytotoxicity assay 72 hrs Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM. 21341674
DU145 Cytotoxicity assay 72 hrs Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM. 21341674
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay, IC50 = 0.22 μM. 21341674
H69AR Cytotoxicity assay 72 hrs Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.25 μM. 21341674
HEK293 Inhibition of human 1.5 mins Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50 = 2.1 μM. 23241029
HEK293 Inhibition of human 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 2.7 μM. 23241029
MDCK2 Inhibition of human 5 mins Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50 = 4.3 μM. 23241029
HEK293 Inhibition of human 1.5 mins Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 7.9 μM. 23241029
HEK293 Inhibition of human 3 mins Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 20.8 μM. 23241029
H3347 Cytotoxicity assay 72 hrs Cytotoxicity against human H3347 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 7.53 μM. 24583355
DLD1 Cytotoxicity assay 72 hrs Cytotoxicity against human DLD1 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 25.1 μM. 24583355
DU145 Cytotoxicity assay 72 hrs Cytotoxicity against human DU145 cells after 72 hrs by SRB assay, IC50 = 9.3 μM. 25003995
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 9.5 μM. 25003995
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 9.8 μM. 25003995
MDA-MB-435 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 6.3 μM. 26226379
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 18.6 μM. 26226379
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 20.1 μM. 26226379
HCT116 Antiproliferative assay 24 to 72 hrs Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by SRB assay, IC50 = 2 μM. 26595875
RKO Antiproliferative assay 24 to 72 hrs Antiproliferative activity against human RKO cells after 24 to 72 hrs by SRB assay, IC50 = 6.2 μM. 26595875
HCT15 Antiproliferative assay 24 to 72 hrs Antiproliferative activity against human HCT15 cells after 24 to 72 hrs by SRB assay, IC50 = 8.5 μM. 26595875
SW480 Antiproliferative assay 24 to 72 hrs Antiproliferative activity against human SW480 cells after 24 to 72 hrs by SRB assay, IC50 = 12.3 μM. 26595875
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 0.8 μM. 26731300
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 0.9 μM. 26731300
T84 Antiproliferative assay 96 hrs Antiproliferative activity against human T84 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 1.2 μM. 26731300
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 1.9 μM. 26731300
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.5 μM. 26841168
A549 Cytotoxicity assay 24 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.8 μM. 26841168
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.9 μM. 26841168
SW480 Cytotoxicity assay 24 hrs Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 1.4 μM. 26841168
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.48 μM. 26994847
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.828 μM. 26994847
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay, IC50 = 7.99 μM. 28285912
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, IC50 = 8.3 μM. 28285912
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay, IC50 = 11.3 μM. 28285912
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, IC50 = 15.6 μM. 28285912
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.3 μM. 28351590
ZR-7530 Antiproliferative assay 72 hrs Antiproliferative activity against human ZR-7530 cells after 72 hrs by MTT assay, IC50 = 18 μM. 28351590
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 20 μM. 28351590
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM. 28789891
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.31 μM. 28789891
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.32 μM. 28789891
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.56 μM. 28789891
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM. 28927790
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.3 μM. 28927790
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.3 μM. 28927790
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.6 μM. 28927790
Maver2 Antiproliferative assay 72 hrs Antiproliferative activity against human Maver2 cells after 72 hrs by MTT assay, IC50 = 0.74 μM. 29150335
NB4 Antiproliferative assay 72 hrs Antiproliferative activity against human NB4 cells after 72 hrs by MTT assay, IC50 = 1 μM. 29150335
Capan1 Antiproliferative assay 72 hrs Antiproliferative activity against human Capan1 cells after 72 hrs by SRB assay, IC50 = 1.5 μM. 29150335
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay, IC50 = 2.4 μM. 29150335
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay, IC50 = 2.8 μM. 29150335
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay, IC50 = 3.8 μM. 29150335
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay, IC50 = 4 μM. 29150335
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells after 72 hrs by SRB assay, IC50 = 4.1 μM. 29150335
U2932 Antiproliferative assay 72 hrs Antiproliferative activity against human U2932 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. 29150335
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50 = 4.8 μM. 29150335
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50 = 5.8 μM. 29150335
A2780/DX Antiproliferative assay 72 hrs Antiproliferative activity against human A2780/DX cells after 72 hrs by SRB assay, IC50 = 20.1 μM. 29150335
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 1.63347 μM. 30115492
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50 = 1.88093 μM. 30115492
KBV1 Cytotoxicity assay Cytotoxicity against human KBV1 cells by MTT method, IC50 = 40 μM. 18771930
KBH5.0 Cytotoxicity assay Cytotoxicity against human KBH5.0 cells by MTT method, IC50 = 7.4 μM. 18771930
KB3-1 Cytotoxicity assay Cytotoxicity against human KB3-1 cells by MTT method, IC50 = 0.68 μM. 18771930
NCI60 Growth inhibition assay Growth inhibition of human NCI60 cells by SBR assay, GI50 = 14.1254 μM. 21035334
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by SRB assay, IC50 = 9.3 μM. 23102893
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by SRB assay, IC50 = 9.48 μM. 23102893
KB Cytotoxicity assay Cytotoxicity against human KB cells by SRB assay, IC50 = 9.83 μM. 23102893
colon cancer cells Cytotoxicity assay Compound was tested in vitro for cytotoxicity against HCT116, human colon cancer cells (taxol-resistant) at a drug concentration producing 50% inhibition of colony formation, ID50 = 0.54 μM. 11965362
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
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
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 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: Orthogonal 3D viability screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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: Orthogonal 3D viability screen for MG 63 (6-TG R) 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
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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 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
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 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
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
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生物活性

产品描述 Irinotecan HCl Trihydrate是伊立替康的盐酸盐三水合物,伊立替康是一种拓扑异构酶 I 抑制剂,对 LoVo 细胞和 HT-29 细胞的 IC50 分别为 15.8 和 5.17 μM。
特性 Irinotecan是一种用于治疗转移性结直肠癌的前药。
靶点
Topo I [1]
体外研究(In Vitro)
体外研究活性 Irinotecan被羧酸酯酶活化为SN-38,从而能够与其靶点,拓扑异构酶I相互作用。IC50浓度下的Irinotecan在LoVo细胞和HT-29细胞系中诱导相似量的可裂解复合物。SN-38诱导可裂解复合物浓度依赖性形成,这在LoVo细胞和HT-29细胞系中没有明显差异。Irinotecan引起的细胞积聚显著不同,在HT-29细胞中的水平始终高于LoVo细胞。[1] Irinotecan的内酯E环和SN-38在水溶液中可逆水解,内酯形式和羧酸盐形式之间的互变取决于PH和温度。Irinotecan主要通过肝脏活化为SN-38。对于相同浓度的Irinotecan和SN-38葡糖苷酸,在肿瘤和正常组织中,β-葡糖醛酸酶介导的SN-38产率均高于Irinotecan 形成的SN-38产率。[2] Irinotecan在肠道,血浆和肿瘤组织中转化为SN-38。[3] Irinotecan在SCLC细胞系中的活性显著高于NSCLC细胞系,而在组织学分型中没有观察到SN-38有明显的差异。[4]
细胞实验 细胞系 LoVo 和HT-29 细胞
浓度 0 μM -100 μM
孵育时间 48小时
方法

指数生长的细胞(LoVo和HT-29细胞)以每种细胞系的最佳接种数量(LoVo 细胞2×10<sup>4</sup>;HT-29细胞10<sup>5</sup>)接种于20 cm<sup>2</sup> Petri培养皿。2天后,用逐渐增加浓度的Irinotecan或SN-38处理一个细胞倍增时间(LoVo 细胞24小时,HT-29细胞40 小时)。0.15 M NaCl洗涤后,细胞进一步在正常培养基中生长两个倍增时间,从胰蛋白酶-EDTA的支撑物中分离,并在血细胞计数器上计数。IC50值的估算如下:与不含Irinotecan 或SN-38培养的细胞相比,引起50%生长抑制的Irinotecan 或SN-38浓度。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2 NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1 AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K 29237470
Immunofluorescence NFκB 22206574
Growth inhibition assay Cell viability 25973791
体内研究(In Vivo)
体内研究活性 在COLO320异种移植物中,Irinotecan诱导92%的最大生长抑制。[5]单剂量Irinotecan显著增加胃,十二指肠,结肠和肝脏中拓扑异构酶I与DNA的共价结合数量。同时,与对照组相比,Irinotecan治疗组的结肠黏膜细胞中DNA链断裂数量明显较高。[6]
动物实验 Animal Models 负荷COLO 320和WiDr异种移植物的雌性裸鼠
Dosages 20 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05854498 Recruiting
Metastatic Colorectal Cancer
University of Wisconsin Madison|Ipsen
October 13 2023 Phase 2
NCT05732129 Not yet recruiting
Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer
Fudan University
March 1 2023 Phase 2
NCT05731518 Recruiting
Small Cell Lung Cancer
Biocity Biopharmaceutics Co. Ltd.
February 23 2023 Phase 1|Phase 2
NCT06003998 Recruiting
Colorectal Cancer|Peritoneal Metastases
Catharina Ziekenhuis Eindhoven
December 27 2022 Phase 2
NCT05277766 Recruiting
Peritoneal Carcinomatosis|Peritoneal Metastases|Colorectal Cancer|Small Bowel Cancer|Appendix Cancer|Gastric Cancer|Pancreatic Cancer|Bile Duct Cancer
University Hospital Ghent|Kom Op Tegen Kanker|University Ghent
November 21 2022 Phase 1
NCT05379790 Recruiting
Gastric Cancer|Peritoneal Metastases
Erasmus Medical Center
May 25 2022 Phase 1

化学信息&溶解度

分子量 677.18 分子式

C33H38N4O6.HCl.3H2O

CAS号 136572-09-3 SDF Download Irinotecan HCl Trihydrate SDF
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 147.67 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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