PX-866

PX-866 potently inhibited purified phosphoinositide and PddIns-3-kinase signaling as assessed by phospho-Ser473-Akt levels in HT-29 colon cancer cells. PX-866 showed antitumor activity in vivo against s.c. A-549 human lung cancer xenografts and OvCar-3 human ovarian cancer in immunodeficient mice. PX-866 also enhanced the antitumor activity of cisplatin against A-549 xenografts and radiation treatment against OvCar-3 xenografts. PX-866 appears to inhibit tumor growth by blocking the phosphatidylinositol 3-kinase (PI3K) pathway and cell motility. The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensionalcultures.