MRTX-9768 是一种有效的、选择性的、具有口服活性的PRMT5-MTA复合体抑制剂,可选择性靶向 MTAP/CDKN2A 缺失的肿瘤。
产品描述
MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
体外活性
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).
体内活性
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].
Cas No.
2629314-68-5
储存和溶解度
DMSO:35 mg/ml(82.46 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years