PI-540

PI-540 is a bicyclic thienopyrimidine derivative that functions as an orally active inhibitor of phosphoinositide 3-kinases (PI3K). Demonstrating potent anti-cancer cell proliferation activity, PI-540 selectively inhibits various PI3K isoforms with IC50 values of 10 nM for P110α, 3510 nM for P110β, 410 nM for P110δ, and 33110 nM for P110γ. In addition to its PI3K inhibition, PI-540 also targets mTOR and DNA-PK, with IC50 values of 61 nM and 525 nM, respectively, making it a valuable tool for cancer research and therapeutic development.