Silatecan (formerly AR-67) is a synthetic, highly lipophilic analogue of camptothecin, with potential antineoplastic and radiosensitizing activities. Silatecan DB-67 binds to and stabilizes the topoisomerase I-DNA covalent complex, inhibiting the religation of topoisomerase I-mediated single-stranded DNA breaks and producing lethal double-stranded DNA breaks when encountered by the DNA replication machinery; inhibition of DNA replication and apoptosis follow. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. References: Arnold SM, Rinehart JJ, Tsakalozou E, Eckardt JR, Fields SZ, Shelton BJ, DeSimone PA, Kee BK, Moscow JA, Leggas M. A phase I study of 7-t-butyldimethylsilyl-10-hydroxycamptothecin in adult patients with refractory or metastatic solid malignancies. Clin Cancer Res. 2010 Jan 15;16(2):673-80. Epub 2010 Jan 12. PubMed PMID: 20068096; PubMed Central PMCID: PMC2831464.

纯度：≥98%

CAS：220913-32-6