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