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Background Information:
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.
Reference:
1. A. W. Hird, et al, Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC AZD5991: A potent and selective macrocyclic inhibitor of Mcl-1 for treatment of hematologic cancers, In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr DDT01-02. doi:10.1158/1538-7445.AM2017-DDT01-02. *Binding potency is measured for its ability to displace BAK peptide from Mcl1-BAK complex, performed by an outside independent third party.
APIM050018: AZD5991
CAS No.: 2143061-81-6.
Molecular Formula: C35H34ClN5O3S2.
Molecular Weight: 672.3 (refer to Certificate of Analysis, batch-specific).
Purity: 99.8-100% Chemically and Atropisomerically Pure by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Elemental Analysis, Binding Potency Reports.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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