Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor ofmyeloid leukemia 1 (MCL-1)inhibitor, with aK_iof 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptoticBCL-2 familymembers. Murizatoclax can be used for the research ofcancer^[1][2].

AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour^[2].

Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts^[2].
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^[2].

765.44

Solid

C₄₂H₅₇ClN₄O₅S

2245848-05-7

Room temperature in continental US; may vary elsewhere.

DMSO : 10 mg/mL(13.06 mM;Need ultrasonic)

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