This study has performed experiments to evaluate the antitumor efficacy of different novel targeted agents on preclinical nasopharyngeal carcinoma models. Three subtypes of experiments were performed: 1) in-vitro drug testing, 2) in-vivo drug testing, and 3) molecular mechanisms of the drug on NPC. Dataset includes both raw and processed data of in-vitro, in-vivo, and molecular experiments performed in this study. The dataset will be accessible once the data are published. File types are easily opened with the both openly accessible or commercial softwares. Details of the file types and softwares used to open are described in the readme file.