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ARN-21934

CAS No. : 2230854-93-8

MCE 站：ARN-21934

产品活性：ARN-21934 是一种有效的，高选择性的，具有血脑屏障 (BBB) 通透性的人拓扑异构酶 II α (human topoisomerase II α) 的抑制剂。与抗癌试剂依托泊苷 (Etoposide; IC₅₀=120 μM) 相比，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，是一种很有前途的抗癌先导化合物。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: 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.

In Vivo: 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

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