AZD5991 is a potent and selective BH3-groove-binding Mcl-1 inhibitor with sub-nanomolar affinity for the target. It demonstrates all the hallmarks of a true Mcl-1 inhibitor: 1. potent, selective, and rapid apoptosis in Mcl-1-dependent cell lines (e.g., GI50 as low as 10 nM in multiple myeloma cell lines); 2. loss of activity upon overexpression of Bcl-xL or siRNA-mediated knockout of Bak; 3. Mcl-1:Bak complex disruption as demonstrated by co-immunoprecipitation. AZD5991 is active in vivo, with complete (100%) tumor regression demonstrated in several mouse xenograft models after a single tolerated dose.

KEYWORDS: AZD5991 | Supplier | BH3-Groove binding Mcl-1 inhibitor | AZD-5991 | AZD 5991 | CT-A5991 | CAS [2143061-81-6] | Non Selective | Mcl-1 | Inhibitor | Proteins