2245848-05-7

2245848-05-7 structure

Name: Murizatoclax
Chemical Name: Murizatoclax
CAS Number: 2245848-05-7
Molecular Formula: C₄₂H₅₇ClN₄O₅S
Molecular Weight: 765.44
Catalog: Signaling Pathways Apoptosis Bcl-2 Family
Create Date: 2021-09-15 17:21:44
Modify Date: 2024-01-06 08:51:46
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].

Name	Murizatoclax

Description	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].
Related Catalog	Signaling Pathways >> Apoptosis >> Bcl-2 Family Research Areas >> Cancer
Target	MCL1:15 pM (Ki)
In Vitro	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].
In Vivo	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].
References	[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.

Molecular Formula	C₄₂H₅₇ClN₄O₅S
Molecular Weight	765.44