ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。

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).

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].

2230854-93-8

C21H24N6

360.46

DMSO:8.33 mg/mL (23.11 mM),ultrasonic and warming and heat to 80°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years