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Overview
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Background
VU661013 is a novel, potent, selective MCL-1 inhibitor (Ki of 97 ± 30 pM).[1]
MCL-1, an anti-apoptotic BCL-2 family member, is commonly upregulated in acute myeloblastic leukemia (AML) cells. Targeting anti-apoptotic proteins in AML is a key therapeutic strategy, and MCL-1 is a critical anti-apoptotic oncoprotein. [1]
VU661013 reduced expansion of multiple AML cell lines in vitro. Venetoclax (a BCL-2 inhibitor) and VU661013 exhibited favorable synergy in several of AML cells lines, venetoclax-resistant AML cells were sensitive to VU661013. [1]
VU661013 decreased tumor growth in an in vivo murine model. VU661013 (25mg/kg) and venetoclax (15mg/kg) can be synergistic in patient-derived xenograft transplantation models. [1]
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- Properties
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Overview