Asulacrine (isethionate)

Asulacrine isethionate (CI-921 isethionate) is a derivative of Amsacrine (HY-13551), a Topoisomerase II inhibitor and an anticancer agent. Asulacrine isethionate binds to DNA via intercalation, forming stable complexes with long residence times at DNA sites. Asulacrine isethionate mediates DNA breakage and DNA-protein cross-linking. Asulacrine isethionate exhibits anticancer activity against leukemia or lung cancer. Asulacrine isethionate can be used in research related to breast cancer, lung cancer, mouse solid tumors and leukemia^[1][2][3][4]. In Vitro:The IC₅₀ values of Asulacrine isethionate against the T-47D breast cancer cell line and the murine leukemia P388/ADR cell line are 6.7 nM and 800 nM, respectively^[4]. In Vivo:Asulacrine (isethionate) (30 mg/kg; i.v.; single dose) administered as a nanocrystalline suspension in male C57BL/6 mice results in reduced peak plasma concentrations, prolonged plasma residence time, and significantly higher drug exposure in liver, lung, and kidney compared to the Asulacrine solution^[1].