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MRTX9768
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRTX9768图片
CAS NO:2629314-68-5
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
MRTX9768 是一种有效的,具有口服活性的 PRMT5 抑制剂。MRTX9768 设计用于结合 PRMT5-MTA 复合物,选择性靶向 MTAP/CDKN2A 缺失的肿瘤。
Cas No.2629314-68-5
分子式C24H17FN6O
分子量424.43
溶解度DMSO : 30 mg/mL (70.68 mM; ultrasonic and warming and heat to 60°C)
储存条件-20°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors[1].

MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].

In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors[1].

[1]. Christopher R. et al. Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr LB003.