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Background Information:
BMS-986158 is an orally bioavailable, potent and domain-selective BET protein inhibitor, binding to the acetyl-lysine binding site of BET bromodomain of BRD4 (Bromodomain-containing 4) with an IC50 < 5nM (FRET) (ref. 1). Display excellent pharmacokinetic properties and efficacy in vitro and in vivo antitumor activity. It is currently in clinical evaluation for advanced solid tumor treatment.
Reference:
1. D. J. Norris, et al, TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS, Patent WO 2015100282.
APIM050025: BMS-986158
CAS No.: 1800340-40-2.
Molecular Formula: C30H33N5O2.
Molecular Weight: 495.6.
Purity: >99.5% chem and optical purity by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 1H-NMR, and Elemental Analysis Report.
Solubility: refer to Certificate of Analysis.
Storage: refer to Certificate of Analysis.
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