Exatecan (DX-8951), a semisynthetic and water-soluble analog of camptothecin, is a potent DNA topoisomerase I inhibitor with antineoplastic activity. It inhibits TOP I with an IC50 of 2.2 μM (0.975 μg/mL) and . Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues.

纯度：≥98%

CAS：171335-80-1