ABT 737-d8

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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、同位素标记物，专注于信号通路和疾病研究领域。
ABT 737-d8 

ABT 737-d8 是 ABT-737 的氘代物。ABT-737 是一种 BH3 模拟物，是一种有效的 Bcl-2、Bcl-xL 和 Bcl-w 抑制剂，EC50 分别为 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 诱导 BCL-2/BAX 复合物的破坏和 BAK 依赖性但不依赖 BIM 的内在凋亡途径激活。ABT-737 诱导自噬，并且具有用于急性髓系白血病 (AML) 研究的潜力。

ABT 737-d8

ABT 737-d8 Chemical Structure

CAS No. : 1217686-68-4

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生物活性

ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

821.48

Formula

C42H37D8ClN6O5S2
CAS 号

1217686-68-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88.

    [3]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81.

    [4]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3.

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