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Irinotecan HCl Trihydrate

別名: CPT-11 HCl Trihydrate 中文名稱：鹽酸依立替康三水合物

Irinotecan HCl Trihydrate是伊立替康的鹽酸鹽三水合物，伊立替康是一種拓?fù)洚悩?gòu)酶 I 抑制劑，對(duì) LoVo 細(xì)胞和 HT-29 細(xì)胞的 IC50 分別為 15.8 和 5.17 μM。

Irinotecan HCl Trihydrate Chemical Structure

Irinotecan HCl Trihydrate Chemical Structure

CAS: 136572-09-3

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1545.43 現(xiàn)貨
5mg 571.52 現(xiàn)貨
25mg 1722.94 現(xiàn)貨
100mg 4332.51 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Irinotecan HCl Trihydrate相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Topoisomerase Signaling Pathways

Topoisomerase信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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

產(chǎn)品描述 Irinotecan HCl Trihydrate是伊立替康的鹽酸鹽三水合物，伊立替康是一種拓?fù)洚悩?gòu)酶 I 抑制劑，對(duì) LoVo 細(xì)胞和 HT-29 細(xì)胞的 IC50 分別為 15.8 和 5.17 μM。
特性 Irinotecan是一種用于治療轉(zhuǎn)移性結(jié)直腸癌的前藥。
靶點(diǎn)
Topo I [1]
體外研究(In Vitro)
體外研究活性 Irinotecan被羧酸酯酶活化為SN-38，從而能夠與其靶點(diǎn)，拓?fù)洚悩?gòu)酶I相互作用。IC50濃度下的Irinotecan在LoVo細(xì)胞和HT-29細(xì)胞系中誘導(dǎo)相似量的可裂解復(fù)合物。SN-38誘導(dǎo)可裂解復(fù)合物濃度依賴性形成，這在LoVo細(xì)胞和HT-29細(xì)胞系中沒有明顯差異。Irinotecan引起的細(xì)胞積聚顯著不同，在HT-29細(xì)胞中的水平始終高于LoVo細(xì)胞。[1] Irinotecan的內(nèi)酯E環(huán)和SN-38在水溶液中可逆水解，內(nèi)酯形式和羧酸鹽形式之間的互變?nèi)Q于PH和溫度。Irinotecan主要通過肝臟活化為SN-38。對(duì)于相同濃度的Irinotecan和SN-38葡糖苷酸，在腫瘤和正常組織中，β-葡糖醛酸酶介導(dǎo)的SN-38產(chǎn)率均高于Irinotecan 形成的SN-38產(chǎn)率。[2] Irinotecan在腸道，血漿和腫瘤組織中轉(zhuǎn)化為SN-38。[3] Irinotecan在SCLC細(xì)胞系中的活性顯著高于NSCLC細(xì)胞系，而在組織學(xué)分型中沒有觀察到SN-38有明顯的差異。[4]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 LoVo 和HT-29 細(xì)胞
濃度 0 μM -100 μM
孵育時(shí)間 48小時(shí)
方法

指數(shù)生長(zhǎng)的細(xì)胞(LoVo和HT-29細(xì)胞)以每種細(xì)胞系的最佳接種數(shù)量(LoVo 細(xì)胞2×10<sup>4</sup>；HT-29細(xì)胞10<sup>5</sup>)接種于20 cm<sup>2</sup> Petri培養(yǎng)皿。2天后，用逐漸增加濃度的Irinotecan或SN-38處理一個(gè)細(xì)胞倍增時(shí)間(LoVo 細(xì)胞24小時(shí)，HT-29細(xì)胞40 小時(shí))。0.15 M NaCl洗滌后，細(xì)胞進(jìn)一步在正常培養(yǎng)基中生長(zhǎng)兩個(gè)倍增時(shí)間，從胰蛋白酶-EDTA的支撐物中分離，并在血細(xì)胞計(jì)數(shù)器上計(jì)數(shù)。IC50值的估算如下：與不含Irinotecan 或SN-38培養(yǎng)的細(xì)胞相比，引起50%生長(zhǎng)抑制的Irinotecan 或SN-38濃度。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在COLO320異種移植物中，Irinotecan誘導(dǎo)92%的最大生長(zhǎng)抑制。[5]單劑量Irinotecan顯著增加胃，十二指腸，結(jié)腸和肝臟中拓?fù)洚悩?gòu)酶I與DNA的共價(jià)結(jié)合數(shù)量。同時(shí)，與對(duì)照組相比，Irinotecan治療組的結(jié)腸黏膜細(xì)胞中DNA鏈斷裂數(shù)量明顯較高。[6]
動(dòng)物實(shí)驗(yàn) Animal Models 負(fù)荷COLO 320和WiDr異種移植物的雌性裸鼠
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

化學(xué)信息&溶解度

分子量 677.18 分子式

C33H38N4O6.HCl.3H2O
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (147.67 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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