Background: GLUTs (glucose transporters) mediates the absorbing of glucose in mammal cells. However, the potential application of GLUT inhibitors in HCC (hepatocellular carcinoma) is largely unknown. Objective: To identify the in vivo activity of GLUT-1 inhibitor BAY-876 on hepatocellular carcinoma cells using PET (positron emission computed tomography). Methods: The expression of GLUT-1 in HCC cell line was identified by qPCR. MGCC-97H cells, which express highest GLUT-1, were injected to nude mice. After 2-3 weeks growth, mice were treated with control (PBS) or 5mg/kg BAY-876 once per day for three days. Mice were injected with 200μCi 18F-FDG and analyzed by PET. Results: MHCC-97H expresses highest GLUT-1 than other cell lines. Treatment of BAY-876 attenuates the absorbing of 18F-FDG in MHCC-97H cells. Conclusion In inhibitor of GLUT-1, BYA-876, could inhibit the absorbing of glucose in HCC cells. This work established a method to identify the in vivo activity of GLUTs inhibitor.