Home DNA Damage/DNA Repair Topoisomerase inhibitor Irinotecan HCl Trihydrate For research use only.

Irinotecan HCl Trihydrate

Synonyms: CPT-11 HCl Trihydrate

Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively.

Irinotecan HCl Trihydrate Chemical Structure

Irinotecan HCl Trihydrate Chemical Structure

CAS: 136572-09-3

Selleck's Irinotecan HCl Trihydrate has been cited by 84 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8402 Cytotoxicity assay 4 days Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment. IC50=0.57 μM 12747798
Hep3B Antiproliferative assay 72 hrs Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM. 19796956
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM. 19796956
NCI60 Growth inhibition assay Growth inhibition of human NCI60 cells by SBR assay, GI50 = 14.1254 μM. 21035334
Hep3B Growth inhibition assay 72 hrs Growth inhibition of human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 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
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
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay, GI50 = 5 μM. 22867019
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay, GI50 = 7.1 μM. 22867019
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
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs, GI50 = 1.9 μM. 25420175
A549 Antitumor assay 4 hrs Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50 = 6.528 μM. 18207748
LOVO Antitumor assay 4 hrs Antitumor activity against human LOVO cells after 4 hrs by MTT assay, IC50 = 9.015 μM. 18207748
MCF7 Antitumor assay 4 hrs Antitumor activity against human MCF7 cells after 4 hrs by MTT assay, IC50 = 17.403 μM. 18207748
LS174T Cytotoxicity assay 96 hrs Cytotoxicity against human LS174T cells after 96 hrs by MTT assay, IC50 = 1.16 μM. 18513976
KB3-1 Cytotoxicity assay Cytotoxicity against human KB3-1 cells by MTT method, IC50 = 0.68 μM. 18771930
KBH5.0 Cytotoxicity assay Cytotoxicity against human KBH5.0 cells by MTT method, IC50 = 7.4 μM. 18771930
KBV1 Cytotoxicity assay Cytotoxicity against human KBV1 cells by MTT method, IC50 = 40 μM. 18771930
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
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.61 μM. 20371183
LoVo Cytotoxicity assay 72 hrs Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50 = 4.99 μM. 20371183
A549 Cytotoxicity assay 3 days Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50 = 6.4 μM. 20942490
LoVo Cytotoxicity assay 3 days Cytotoxicity against human LoVo cells after 3 days by MTT assay, IC50 = 8.8 μM. 20942490
MDA-MB-435 Cytotoxicity assay 3 days Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay, IC50 = 17 μM. 20942490
A375 Cytotoxicity assay 72 hrs Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM. 21341674
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
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
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 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
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
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
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
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
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
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
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
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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Biological Activity

Description Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively.
Features Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets
Topo I [1]
In vitro
In vitro Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. [1] The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. [2] Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. [3] Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. [4]
Cell Research Cell lines LoVo and HT-29 cells
Concentrations 0 μM -100 μM
Incubation Time 48 hours
Method

Exponentially growing cells (LoVo and HT-29 cells) are seeded in 20 cm2 Petri dishes with an optimal cell number for each cell line (2 × 104 for LoVo cells, 105 for HT-29 cells). They are treated 2 days later with increasing concentrations of Irinotecan or SN-38 for one cell doubling time (24 hours for LoVo cells, 40 hours for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.
Experimental Result Images Methods Biomarkers Images 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
In Vivo
In vivo In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. [5] A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group. [6]
Animal Research Animal Models Female nude mice with COLO 320 and WiDr xenografts.
Dosages 20 mg/kg
Administration Intraperitoneal injection
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

Chemical lnformation & Solubility

Molecular Weight 677.18 Formula

C33H38N4O6.HCl.3H2O
CAS No. 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
Storage (From the date of receipt)

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DMSO : 100 mg/mL ( (147.67 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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