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「同位素标记抑制剂」SAR405838-d10
生物活性:SAR405838-d10 (MI-77301-d10) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity[1][2][3].
体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量:572.56
Formula:C29H24D10Cl2FN3O3
非标记 CAS:1303607-60-4
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.
纯度 & 产品资料
Data Sheet (538 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-220.
[Content Brief]
[2]. Wang S, et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-5865.
[Content Brief]
[3]. Hoffman-Luca CG, et al. Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo. Clin Cancer Res. 2015 Jun 1;21(11):2558-2568.
[Content Brief]
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