上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
ARN-21934 纯度: 98.02%
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。
ARN-21934 Chemical Structure
CAS No. : 2230854-93-8
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥3850 | In-stock | |
5 mg | ¥3500 | In-stock | |
10 mg | ¥5800 | In-stock | |
25 mg | ¥11000 | In-stock | |
50 mg | ¥17000 | In-stock | |
100 mg | ¥25000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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ARN-21934 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Cell Cycle/DNA Damage Compound Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Anti-Lung Cancer Compound Library
- Anti-Blood Cancer Compound Library
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[1]. |
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IC50 & Target[1] |
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体外研究 (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[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 IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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[1] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
360.46 |
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Formula |
C21H24N6 |
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CAS 号 |
2230854-93-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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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
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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。 |
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参考文献 |
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