Irinotecan, Hydrochloride Salt, Trihydrate ([1,4

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.\n\nSolubility:\nSoluble in DMSO at 100mg/ml; very poorly soluble in ethanol; soluble in water at 25mg/ml; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

I8611-02

Size

100mg

Form

Supplied as a pale yellow powder.

Purity

~99%

References

1. 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). 2. Rothenberg, M.L. \"Topoisomerase I inhibitors: Review and update.\" Ann. Oncol. 8:837-855 (1997). 3. 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). 4. Fuchs, C., et al. \"Irinotecan in the treatment of colorectal cancer.\" Cancer Treat. Rev. 32:491-503 (2006). 5. Kaneda, N., et al. \"Metabolism and pharmacokinetics of the camptothecin analogue CPT-11 in the mouse.\" Cancer Res. 50:1715-1720 (1990). 6. 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). 7. 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).