I-4122 Irinotecan, Hydrochloride Salt, Trihydrate, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; very poorly soluble in ethanol; soluble in water at 25 mg/mL; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

RCN-107 RCN-106 RCN-105 RCN-104 RCN-103 RCN-102 RCN-101

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• Irinotecan (CPT-11) is a topoisomerase I inhibitor. It is a semisynthetic analog of the natural alkaloid camptothecin and has an active metabolite SN-38 (7-Ethyl-10-hydroxycamptothecin). During the S phase of the cell cycle, camptothecins selectively bind to and stabilize topoisomerase I-DNA complexes, inhibiting religation, causing the accumulation of topoisomerase I-mediated single-strand DNA breaks in the DNA, and producing irreversible double-strand DNA breaks that lead to cell death. Garcia-Carbonero, R. and Supko, J.G. "Current perspectives on the clinical experience, pharmacology, and continued development of the camptothecins." Clin. Cancer Res. 8: 641-661 (2002).
• Both irinotecan and topotecan have activity in vivo against L1210 and P388 leukemia, mouse colon adenocarcinomas 38 and 51, Lewis lung carcinoma, mouse breast adenocarcinoma 16/C, and human tumor xenografts of B16 melanoma and HT-29 colon adenocarcinoma. Rothenberg, M.L. "Topoisomerase I inhibitors: Review and update." Ann. Oncol. 8: 837-855 (1997).
• In the human tumor stem cell assay, irinotecan has activity in vitro against colorectal, non-small cell lung, ovarian, breast, mesothelioma, pancreas, sarcoma, and cervical cancers at low drug concentrations. Shimada, Y., et al. "Activity of CPT-11 (irinotecan hydrochloride), a topoisomerase I inhibitor, against human tumour colony-forming units." Anticancer Drugs 5: 202-206 (1994).
• Irinotecan is used to treat patients with colorectal cancer. Fuchs, C., et al. "Irinotecan in the treatment of colorectal cancer." Cancer Treat. Rev. 32: 491-503 (2006).
• Irinotecan is activated by hydrolysis to its active metabolite SN-38. Kaneda, N., et al. "Metabolism and pharmacokinetics of the camptothecin analogue CPT-11 in the mouse." Cancer Res. 50: 1715-1720 (1990). Kawato Y., et al. "Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11." Cancer Res. 51: 4187-4191 (1991).
• SN-38 is inactivated by the enzyme UGT1A1 by glucuronidation. Iyer, L., et al. "Genetic predisposition to the metabolism of irinotecan (CPT-11). Role of uridine diphosphate glucuronosyltransferase isoform 1A1 in the glucuronidation of its active metabolite (SN-38) in human liver microsomes." J. Clin. Invest. 101: 847-854 (1998).
• Water content may vary slightly from lot to lot. Please refer to the elemental analysis of each lot for the water content.
• Irinotecan is the active ingredient in the drug sold under the trade name Camptosar® in USA and Campto® in Japan.  This drug has been approved in at least one country for use in patients with metastatic colorectal cancer. NOTE: THE IRINOTECAN SOLD BY LC LABORATORIES FOR RESEARCH IS NOT COMPTOSAR® OR CAMPTO®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.