PF-04691502

PI3Kα、-β、-δ、-γ和mTOR抑制剂（对于人类酶，Kis分别为1.8、2.1、1.6、1.9和16nM）；降低BT-20、SKOV3和U87MG细胞的增殖（IC50分别为313、188和179nM）；在2.5和5µM时抑制HUVEC的毛细血管形成和迁移；在500和1,000nM时诱导U87MG细胞在G1期细胞周期停滞；在每天10mg/kg时减少NCIH1650和H1975NSCLC小鼠异种移植模型中的肿瘤体积。A PI3Kα, -β, -δ, -γ, and mTOR inhibitor (Kis = 1.8, 2.1, 1.6, 1.9, and 16 nM, respectively, for the human enzymes); decreases the proliferation of BT-20, SKOV3, and U87MG cells (IC50s = 313, 188, and 179 nM, respectively); inhibits capillary tube formation by, and migration of, HUVECs at 2.5 and 5 µM; induces cell cycle arrest at the G1 phase in U87MG cells at 500 and 1,000 nM; decreases tumor volume in NCI H1650 and H1975 NSCLC mouse xenograft models at 10 mg/kg per day.