MRTX9768

MRTX9768CAS号: 2629314-68-5分子式: C24H17FN6O分子量: 424.43描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:35 mg/ml(82.46 mM)
生物活性
靶点
SDMA:3 nM(HCT116 MTAP-del cells), SDMA:544 nM(HCT116 MTAP-WT cells), cell proliferation:11 nM(HCT116 MTAP-del cells), cell proliferation:861 nM(HCT116 MTAP-WT cells)
In vitro(体外研究)
MRTX-9768, a potent inhibitor of 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).
In vivo(体内研究)
In xenograft studies, oral administration of MRTX-9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1].