Objective:To explore effects of PI3K/mTOR dual inhibitor NVP-BEZ235 on proliferation and apoptosis in nasopharyngeal carcinoma (NPC). Methods:We treated NPC cells CNE1 and SUNE1 with NVP-BEZ235 in different concentrations,MTT assay was used to detect inhibition of cell proliferation by NVP-BEZ235. Inhibitors-induced apoptosis in NPC cells was evaluated by propidium iodide (PI)staining assay,4＇,6-diamidino-2-phenylindole (DAPI)staning and Transferase-mediated FITC-12-dUTP nick-end labeling (TUNEL)assay. Western blot analysis was used to detect the proteins of PI3K/mTOR pathway. Tumor xenografts were established by injection of CNE1 cells into nude mice to observe the growth inhibitory effect by NVP-BEZ235 and effects of the inhibitor on PI3K/mTOR pathway and apoptosis in vivo. Results:① NVP-BEZ235 selectively inhibited proliferation of NPC cells rather than normal nasopharyngeal cells. ② NVP-BEZ235 selectively inhibited the phosphorylation of PI3K/mTOR downstream signal molecules. ③ Exposure of NPC cells to NVP-BEZ235 resulted in G1 growth arrest and significant apoptosis. ④ In CNE1 nude mice xenograft models,orally NVP-BEZ235 efficiently attenuated tumor growth and shrinked tumor volumes,and induced apoptosis through blocking phosphorylation of PI3K/mTOR downstream molecules in vivo. Conclusion:NVP-BEZ235 selectively inhibited proliferation of NPC cells and induced apoptosis through G1 growth arrest and inhibiting the phosphorylation of PI3K/mTOR downstream signal molecules both in vivo and in vitro.