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
CAS: 136572-09-3
产品质控
批次：
纯度：
99.97%
99.97
Irinotecan HCl Trihydrate相关产品
相关信号通路图
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 | ||
| 点击查看更多细胞系数据 | |||||
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 |
|
| 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1 TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2 |
|
25973791 | |
| 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 |
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 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
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
只
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，注：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：取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：取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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