BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
BET inhibitor CF53 potently inhibits different BET proteins with Kd values of 0.5-2.2 nM, weakly inhibits CREBBP (Ki=47 nM) and shows excellent selectivity over other bromodomain containing proteins.
BET inhibitor CF53 inhibits cell growth in MOLM-13 and MDA-MB-231 cell lines with IC50 of 7 and 85 nM, respectively.
CF53 demonstrates significant antitumor activity in both triple-negative breast cancer and acute leukemia xenograft models in mice.
