SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment.

SF1126 (0.5-2.5 μM; pre-30 minutes) and sorafenib shows that combined treatment of SF1126 and sorafenib blocks multiple key enzymes in PI3K/AKT/mTOR and Ras/Raf/MAPK pathway. SF1126 (1-10 μM; 24 hours) causes cell-cycle arrest with a proportional increase in G0-G1 and a decrease in the number of cells in the S-phase in Hep 3B, Hep G2, SK-Hep1, and Huh7 cells. SF1126 (0-6 μM; 48 hours) inhibits Hep3B, HepG2, SK-Hep1, and Huh7 cell proliferation with IC50s of 5.05, 6.89, 3.14, and 2.14 μM, respectively [1].