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AZD5991 (AZD-5991)
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 (ref 1). It is currently in clinical evaluation for treatment of hematologic cancers.
Catalog NO: CT-A5991
Synonym: AZD-5991
CAS NO: 2143061-81-6
Mol. Formula: C35H34ClN5O3S2
MW: 672.3 (refer to Certificate of Analysis, batch-specific)
** in vivo Quality material. >99% Pure by Achiral and Chiral HPLCs (attached), w/ confirmed binding potency (Ref 2A, 2B). Hemihydrate, validated by a spot-on Quantitative Elemental Analysis. Bulk stock. Prompt.