ARN-21934 is a potent and selective inhibitor for human topoisomerase II α and topoisomerase II β. ARN-21934(IC50 = 2 μM) inhibits DNA relaxation as compared to the anticancer agent Etoposide (IC50=120 μM).

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO:8.33 mg/mL (23.11 mM)

Topo II:2 μM

ARN-21934 is more potent against the α isoform. ARN-21934 exhibits a small panel of human cancer cell lines such as melanoma (A375, IC50 = 12.6 μM and G-361, IC50 = 8.1 μM), breast (MCF7, IC50 = 15.8 μM), endometrial (HeLa, IC50 = 38.2 μM), lung (A549, IC50 = 17.1 μM), and androgen-independent prostate (DU145, IC50 = 11.5 μM) cancer cells[1].

ARN-21934 is able to reach the brain, with a maximum concentration of compound at 60 min, and is still present in the brain 360 min after injection. ARN-21934 (intraperitoneal injection; 10 mg/kg) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life and clearance value are 149 min in circulation and 0.116 L/(min kg)[1].