SF2523 is a potent, dual inhibitor of PI3K and BRD4 with IC50 of 241, 34, 158 nM for BRD4 (BD1), PI3Kα and PI3Kγ, respectively.
SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and BRD4(BD1) (Kd=150 nM), binds more weakly BRD4(BD2) (Kd = 710 nM).
SF2523 blocks MYC expression and activation, promotes MYC degradation, and markedly inhibits cancer cell growth and metastasis both in vitro and in vivo.
