MRTX9768 hydrochloride
MRTX9768 hydrochloride 是一种有效的，具有口服活性的 PRMT5 抑制剂。MRTX9768 hydrochloride可结合 PRMT5-MTA 复合体。
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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: ajcx34980
- CAS: N/A
- 别名:
- 分子式: C24H18ClFN6O
- 分子量: 460.89
- 纯度: ＞98%
- 溶解度: DMSO : 90 mg/mL (195.27 mM; Need ultrasonic)|Water : 40 mg/mL (86.79 mM; Need ultrasonic)
- 储存: -20°C, protect from light
- 库存: 现货
Background
MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[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].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1].
In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1].
[1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA.
[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.
