CPI 0610

CPI 0610 is a potent, selective, and cell-active BET bromodomain inhibitor with IC50 of 39 nM for BRD4-BD1 in TR-FRET assay; shows remarkably selectivity, over the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8; has an IC50 of 0.18 uM in MYC RNA expression assay; demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model.

References 1. Albrecht BK, et al. J Med Chem. 2016 Feb 25;59(4):1330-9. 2. Siu KT, et al. Leukemia. 2017 Jan 3. doi: 10.1038/leu.2016.355. View Related Products by Target Bromodomain