Exatecan mesylate (DX8951)

Description: Exatecan mesylate (DX-8951), a semisynthetic and water-soluble analog of camptothecin, is a potent DNA topoisomerase I inhibitor with an IC50 of 2.2 uM (0.975 ug/mL) and with antineoplastic activity. 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.

References:

1. Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug; 86(8):776-82.

2. Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1; 63(1):80-5.

3. Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7; 72(4):680-6.

4. Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads. Bioorg Med Chem Lett. 2016 Mar 15; 26(6):1542-5. doi: 10.1016/j.bmcl.2016.02.020. PubMed PMID: 26898815.

Related CAS #: 169869-90-3 (mesylate) 171335-80-1 (free base) 197720-53-9 (mesylate dihydrate) 144008-87-7 (HCl)