Malignant neoplasms exhibit an elevated rate of glycolysis and a high demand for glucose over normal cells. This characteristic can be exploited for in vivo imaging and tumor targeting examined. In this manuscript, we describe the synthesis of near-infrared (NIR) fluorochrome IR-822-labeled 2-amino-2deoxy-o-glucose (DG) for optical imaging of tumors in mice. NIR fluorescent dye IR-820 was subsequently conjugated with 3-Mercaptopropionic acid and 2-amino-2-deoxy-D-glucose to form IR-822-DG. The cell experiments and acute toxicity studies demonstrated the low toxicity of IR-822-DG to normal cells/tissues. The dynamic behavior and targeting ability of IR-822-DG in normal mice was investigated with a NIR fluorescence imaging system. The in vitro and in vivo tumor targeting capabilities of IR-822-DG were evaluated in tumor cells and tumor bearing mice, respectively. Results demonstrated that IR822-DG actively and efficiently accumulated at the site of the tumor. The probe also exhibited good photostability and excellent cell membrane permeability. The study indicates the broad applicability of IR-822-DG for tumors diagnosis, especially in the glucose-related pathologies. (C) 2017 Elsevier Inc. All rights reserved.