Name: Irinotecan
Brand: Selleck Chemicals
SKU: S1198
Rating: 5 (39 reviews)

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

CAS: 97682-44-5

Selleck's Irinotecan has been cited by 39 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Irinotecan Related Products

Related Targets	Topo I Topo II Topo IV	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

Topoisomerase Signaling Pathway

Choose Selective Topoisomerase Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	7%DMSO 1 93%Corn oil	2.1mg/ml (3.58mM)	Taking the 1 mL working solution as an example, add 70 μL of 30 mg/ml clear DMSO stock solution to 930 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	6.0mg/ml (10.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.5mg/ml (0.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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