80841-48-1

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 .

Asulacrine (CI-921) is an orally active DNA intercalating topoisomerase II inhibitor. Asulacrine binds to DNA via intercalation, with its acridine chromophore intercalated between base pairs and substituents located in the major/minor grooves, which stabilizes DNA against acid denaturation. Asulacrine acts as a cell cycle inhibitor, disruptor, and arrest inducer, slowing cell progression in late S/G2 phase, causing G2 phase arrest and inducing unbalanced growth. Asulacrine inhibits cell growth, clonogenicity, and colony formation, and leads to histological destruction of tumor cells. Compared to cells in exponential growth phase, Asulacrine exhibits lower toxicity to quiescent cells; its activity depends on cationic properties, and it has better water solubility and metabolic stability. Asulacrine can be used in research related to leukemia, lung cancer, colon cancer, breast cancer, melanoma, adriamycin-resistant mammary adenocarcinoma, and mouse solid tumors .