AZD5991 (AZD-5991) is a potent and selective macrocyclic inhibitor of Mcl-1 with sub-nanomolar affinity (SPR Kd=0.17 nM).
AZD5991 promotes rapid apoptosis in Mcl-1-dependent cell lines (GI50=10 nM in multiple myeloma cell lines), disrupts Mcl-1/Bak complex.
AZD5991 completely causes tumor regression in several mouse xenograft models after a single tolerated dose.
1. Alexander W. Hird, et al. Abstract DDT01-02: AZD5991: A potent and selective macrocyclic inhibitor of Mcl-1 for treatment of hematologic cancers, AACR. DOI: 10.1158/1538-7445.
