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SN-38 is an inhibitor of topoisomerase I and an active metabolite of the prodrug irinotecan (Item No. 14180).1,2 It is formed from irinotecan by carboxylesterases.1 SN-38 (0.1, 1, and 10 µM) induces topoisomerase I-dependent DNA cleavage in a cell-free assay.2 It induces DNA single-strand breaks in HT-29 colorectal adenocarcinoma cells when used at a concentration of 200 nM and cytotoxicity in HT-29 cells (IC50 = 8.8 nM). SN-38 (100 mg/kg per day) reduces tumor volume without affecting body weight in an MX-1 breast cancer mouse xenograft model.3
WARNING This product is not for human or veterinary use.
1. Lessons learned from the irinotecan metabolic pathway. Curr. Med. Chem. 10(1), 41-49 (2003).
2. Comparison of topoisomerase I inhibition, DNA damage, and cytotoxicity of camptothecin derivatives presently in clinical trials. J. Natl. Cancer Inst. 86(11), 836-842 (1994).
3. Antitumor activity of a camptothecin derivative, CPT-