Irinotecan HCl
Topoisomerase I inhibitor / Irinotecan is a semi-synthetic derivative of camptothecin that is an FDA approved anticancer drug. It is a prodrug that is converted by tissue esterases to 7-ethyl-10-hydroxycamptothecin (SN-38), a potent inhibitor of DNA topoisomerase I.1,2 Although irinotecan is also a topoisomerase inhibitor, SN-38 is approximately 1000 times as potent in purified enzyme studies. In vitro cytotoxicity assays show much greater variability in potency between the two (2-2000 fold).3
Biochemicals & reagents
136572-09-3
1) Kunimoto et al., (1987) Antitumor activity of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin, a novel water-soluble derivative of camptothecin against murine tumors; Cancer Res. 47 5944 / 2) Mathijssen et al., (2002) Pharmacology of topoisomerase I inhibitors irinotecan (CPT-11) and toptecan; Curr.Cancer Drug Targets 253 5892 / 3) Pfizer drug insert
-20°C
TARGET: Topoisomerase; DNA -- PATHWAY: DNA synthesis; Transcription; Cytotoxicity -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer