Irinotecan

Synonyms: (+)-Irinotecan,CPT-11

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

Irinotecan Chemical Structure

Irinotecan Chemical Structure

CAS No. 97682-44-5

Purity & Quality Control

Irinotecan Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cytotoxicity assay 10 μM DMSO ID50=540 nM 11965362
VM46 cytotoxicity assay 10 μM DMSO ID50=220 nM 11965362
MCF-7ADR cytotoxicity assay 10 μM DMSO ID50>500 nM 11965362
L1210 cytotoxicity assay IC50=1.2 µM 1846923
RPMI8402 cytotoxicity assay 100 μM IC50=570 nM 12747798
A-549 cytotoxicity assay ~20 μM DMSO IC50=6.528 μM 18207748
LOVO cytotoxicity assay ~20 μM DMSO IC50=9.015 μM 18207748
MCF7 cytotoxicity assay ~20 μM DMSO IC50=17.403 μM 18207748
LS174T Growth inhibitory assay DMSO IC50=1.16 μM 18479118
KB3-1 cytotoxicity assay IC50=0.68 μM 18771930
KBV-1 cytotoxicity assay IC50=40 μM 18771930
KBH5.0 cytotoxicity assay IC50=7.4 μM 18771930
Hep G2 Growth inhibitory assay ~10 μM DMSO IC50=5.94 μM 19796956
Hep 3B Growth inhibitory assay ~10 μM DMSO IC50=4.73 μM 19796956
Hep 2.2. Growth inhibitory assay ~10 μM DMSO IC50>10 μM 19796956
A549 cytotoxicity assay DMSO IC50=4.61 μM 20371183
MDA-MB-435 cytotoxicity assay DMSO IC50=1.14 μM 20371183
LOVO cytotoxicity assay DMSO IC50=4.99 μM 20371183
MDA-MB-435 cytotoxicity assay DMSO IC50=17 μM 20942490
NCI60 Growth inhibitory assay DMSO GI50=14.1254 μM 21035334
H460 cytotoxicity assay DMSO IC50=0.015 μM 21341674
PC-3 cytotoxicity assay DMSO IC50=0.22 μM 21341674
HT29 cytotoxicity assay DMSO IC50=0.004 μM 21341674
SK-MEL-2 cytotoxicity assay DMSO IC50=0.1 μM 21341674
A375 cytotoxicity assay DMSO IC50=0.004 μM 21341674
Malme-3M cytotoxicity assay DMSO IC50=0.2 μM 21341674
DU 145 cytotoxicity assay DMSO IC50=0.2 μM 21341674
LNCaP cytotoxicity assay DMSO IC50=0.009 μM 21341674
IGROV-1 cytotoxicity assay DMSO IC50=0.03 μM 21341674
KB cytotoxicity assay ~20 μM DMSO IC50=9.83 μM 22079254
KB-vin cytotoxicity assay ~20 μM DMSO IC50>20 μM 22079254
Click to View More Cell Line Experimental Data

Biological Activity

Description Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Features Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets
Topo I [1]
(LoVo, HT-29 cells)
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.

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 Administered via i.p.
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 Information & Solubility

Molecular Weight 586.68 Formula

C33H38N4O6

CAS No. 97682-44-5 SDF Download Irinotecan SDF
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 25 mg/mL ( (42.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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