生物活性:MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1][2].
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]。
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量:571.75
Formula:C33H33D6N7O2
CAS 号:2639608-44-7
非标记 CAS:2206736-04-9
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 (537 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]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.