Murizatoclax

Murizatoclax (AMG 397) 是一种有效，选择性和具有口服活性的髓样白血病 1 (MCL-1) 抑制剂，Ki 值为 15 pM。Murizatoclax 与促凋亡 BCL-2 家族成员竞争性结合 MCL1 的 BH3 结合沟。Murizatoclax 可用于癌症的研究。

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Background

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[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].

[1]. Wang H, et, al. Targeting MCL-1 in cancer: current status and perspectives. J Hematol Oncol. 2021 Apr 21;14(1):67.
[2]. Caenepeel S, et al. Abstract 6218: discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor. Cancer Res. 2020;80(16 Supplement):6218.