MRTX9768
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。
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包装价格促销价数量
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5mg￥10250.008200.00- +
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10mg￥16025.0012820.00- +
- 货号: ajcx34272
- CAS: 2629314-68-5
- 别名:
- 分子式: C24H17FN6O
- 分子量: 424.43
- 纯度: ＞98%
- 溶解度: DMSO : 30 mg/mL (70.68 mM; ultrasonic and warming and heat to 60°C)
- 储存: -20°C, protect from light
- 库存: 现货
Background
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.
