Irinotecan, Hydrochloride Salt, Trihydrate **
產品名稱：Irinotecan, Hydrochloride Salt, Trihydrate
產品貨號：LC I-4122
產品規格：1 G
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, medical, 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.
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
