Abstract: In order to improve in vivotargeting of doxorubicin (Dox) and reduce its toxicity,the targeting ligand 2-deoxy-aminoglucose (AG) was used to modify doxorubicin to form a new anti-tumor drug.The products were charactered by ¹H NMR and MS,and the targeting was investigated by near-infrared imaging.Compared with Dox,the product treating MCF-7 and U87MG cells showed higher antitumor activity in vitro by MTT assay.In conclusion,the modified products effectively enhanced the targeting and pharmacodynamics in contrast with Dox,and it would be a potential therapeutic drug for cancer.