ARN-21934

Research use only, not for human use.

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 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).(In Vitro):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.(In Vivo):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).

ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM.ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively.

ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life is 149 min in circulation, still being present in plasma 360 min after injection. The compound also exhibits good clearance values (0.116 L/(min kg)). Besides, 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

——

Cell Cycle/DNA Damage

Topoisomerase

——

——

——

2230854-93-8

360.46

C21H24N6

>98% (HPLC)

In Vitro:?DMSO : 8.33 mg/mL (23.11 mM)

N/A

——

(-20℃)

With Ice Pack

≥ 2 years