Name: Irinotecan (CPT-11)
Brand: Selleck Chemicals
SKU: S1198
Availability: InStock
Rating: 5 (56 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Other Topoisomerase Inhibitors	Camptothecin (CPT) (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan Eleutherin

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (42.61 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	7%DMSO 1 93%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.100mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Chemical Information, Storage & Stability

Molecular Weight	586.68	Formula	C₃₃H₃₈N₄O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	97682-44-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(+)-Irinotecan,CPT-11			Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7

Mechanism of Action

Features	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I (LoVo, HT-29 cells)
In vitro	Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. This compound 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 this chemical is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of this compound 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 this agent to SN-38. At equal concentrations of this drug and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from this compound in both tumour and normal tissue. It is also converted to SN-38 in intestines, plasma and tumor tissues. This agent is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38.
In vivo	In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. A single dose of this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11914913/ [2] https://pubmed.ncbi.nlm.nih.gov/16842384/ [3] https://pubmed.ncbi.nlm.nih.gov/15182436/ [4] https://pubmed.ncbi.nlm.nih.gov/9649129/ [5] https://pubmed.ncbi.nlm.nih.gov/9033637/ [6] https://pubmed.ncbi.nlm.nih.gov/21046105/ [7] https://pubmed.ncbi.nlm.nih.gov/16317751/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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Irinotecan (CPT-11) Topoisomerase I Inhibitor

Chemical Structure

Molecular Weight: 586.68