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Background Information:
AZD4320 (AZD-4320) is a BH3 mimetic and highly potent dual Bcl-2/Bcl-XL inhibitor with binding affinity in low nanomolar range similar to ABT-263 (Novitoclax), but with a better therapeutic index (lower toxicities) and amenable to I. V. administration (ref 1). It rapidly induces caspase-3 (CC3) cleavage and cell death in both Bcl-2-driven (SuDHL4, GI50 <50 nM) and Bcl-XL-driven (SuDHL8, GI50 <50 nM) diffuse large B-cell lymphoma (DLBCL) cell lines; Achieves complete and sustained (>24 days) tumor regressions in a mouse RS4;11 acute lymphocytic leukemia xenograft model (20 mg/kg, i.v.) (ref 1).
Reference:
1. J. Cidado, et al, AZD4320 is a potent, dual Bcl-2/xLinhibitor that rapidly induces apoptosis in preclinical hematologic tumor models [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 311.
APIM050015: AZD4320
CAS No.: 1357576-48-7.
Molecular Formula: C45H48ClF3N4O7S3?1/2H2O.
Molecular Weight: 954.5.
Purity: 99.9-100% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 19F-, 1H-NMRs, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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