AMG-176

AMG-176 is a potent, selective and orally bioavailable MCL-1 inhibitor, with a Ki of 0.13 nM.

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Research Areas >> Cancer

Mcl-1:0.13 nM (Ki)

AMG-176 is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (Ki=0.13 nM), with potential pro-apoptotic and antineoplastic activities. Upon administration, AMG 176 binds to and inhibits the activity of MCL-1. This disrupts the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes and induces apoptosis in tumor cells[1][2].

[1]. Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387.

[2]. Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142.

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