NSC 727357

NSC 727357 is a DNA intercalator and topoisomerase inhibitor with antitumor activity. NSC 727357 can inhibit cells proliferation and induce G1 phase arrest. NSC 727357 can be used for the research of cancer, such as melanoma^[1]. In Vitro:NSC 727357 (<10 μM) induces Top1 cleavage complexes at specific sites, and inhibits Top1 catalytic activity at high concentrations (≥10 μM); it also induces a limited number of Top2-DNA cleavage complexes^[1].
NSC 727357 intercalates into DNA and supercoils it^[1].
NSC 727357 (0.1-5 μM, 18 h) arrests HT29 cells in the G1 phase of the cell cycle^[1].
NSC 727357 exhibits potent antiproliferative activity in the NCI-60 cell line panel with a GI₅₀ value of 0.067 μM^[1].
In Vivo:NSC 727357 (13.4-30 mg/kg, i.p., starting on day 7 after tumor implantation, daily for 5 days) inhibits tumor growth in nu/nuNCr mice bearing LOX-IMVI melanoma xenografts^[1].