ARN-21934|cas:2230854-93-8|西域试剂

ARN-21934,98.02%

产品编号：Bellancom-137466| CAS NO：2230854-93-8| 分子式：C₂₁H₂₄N₆| 分子量：360.46

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货号	价格	库存与货期
Bellancom-137466	￥3500.00	杭州北京（现货）
Bellancom-137466	￥5800.00	杭州北京（现货）
Bellancom-137466	￥11000.00	杭州北京（现货）
Bellancom-137466	￥17000.00	杭州北京（现货）
Bellancom-137466	￥25000.00	杭州北京（现货）

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ARN-21934

产品介绍

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。

生物活性

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC₅₀ of 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7742 mL	13.8712 mL	27.7423 mL
5 mM	0.5548 mL	2.7742 mL	5.5485 mL
10 mM	0.2774 mL	1.3871 mL	2.7742 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式