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

[Camptosar] [Topotecin] [Campto] [Camptothecin 11] [CPT-11] [U-101440E] [DQ-2805]

M.W. 677.18

C33H38N4O6•HCl•3H2O

[136572-09-3]

RTECS:  DW1060750

M.I. 14:  5091

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

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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).

• 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 is NOT Camptosar® or Campto®, and is NOT for human use.

• Water content may vary slightly from lot to lot.  Please refer to the elemental analysis of each lot for the water content.

• 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.