ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor forhumantopoisomeraseII αover β. ARN-21934 inhibits DNA relaxation with anIC₅₀of 2 μM as compared to the anticancer agent Etoposide (IC₅₀=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research^[1].

ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC₅₀value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM^[1].
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 IC₅₀values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively^[1].

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^[1]

360.46

Solid

C₂₁H₂₄N₆

2230854-93-8

Room temperature in continental US; may vary elsewhere.

DMSO : 8.33 mg/mL(23.11 mM;ultrasonic and warming and heat to 80℃)

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。