bisantrene

Description: Bisantrene (CL 216942 and NSC 337766) is potent inhibitor of topoisomerase II and DNA intercalators. It may be used as model compounds to study P-glycoprotein-mediated multiple drug resistance (MDR1). Bisantrene may be used as a Rac1 inhibitor. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity.

References:

1. Sissi C, et al. DNA-binding preferences of Bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec; 54(6):1036-45.

2. Yap HY, et al. Bisantrene, an active new drug in the treatment of metastatic breast cancer. Cancer Res. 1983 Mar; 43(3):1402-4.

Related CAS #: 78186-34-2 (free base) 71439-68-4 (2HCl) 97910-18-4 (4HCl) 97910-19-5 (nitrate) 97910-20-8 (sulfate) 101218-44-4 (acetate)