Description
Y08060 is a potent and selective BET inhibitor with Kd of 306nM for BRD4 BD1, displays excellent selectivity for BET subfamily over other non-BET family with the exception of moderate inhibition of CBP/EP300; esuppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. such as C4-2B, LNCaP, and 22Rv1; demonstrates good PK profile with high oral bioavailability (61.54%)