AZD5991 CAS NO.2143010-83-5

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AZD5991 is a potent and selective Mcl-1 inhibitor with an IC50 of <3 nM in FRET assay for treatment of hematologic cancers. AZD5991 has high selectivity and affinity for Mcl-1 and is currently in clinical development. AZD5991 shows potent antitumor activity in vivo with complete tumor regression in several models of multiple myeloma and acute myeloid leukemia after a single tolerated dose as monotherapy or in combination with bortezomib or venetoclax. AZD5991 monotherapy caused apoptosis preferentially in hematological cell lines with 6/22 AML and 7/19 MM cell lines showing caspase EC50 values <100 nM. In solid tumor cell lines single agent activity was seen mostly in NSCLC and BrCa.