PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.
PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.
PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.
PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.
PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
