产品
编 号:F741462
分子式:C42H57ClN4O5S
分子量:765.44
产品类型
结构图
CAS No: 2245848-05-7
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产品详情
生物活性:
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer.
体内研究:
Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts.Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively.
体外研究:
AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour.