Objective To explore the in vitro cytotoxicity of sunitinib in highly metastatic hepatocellular carcinoma cell line MHCC97-H, and the effect of it on the expression level of focal adhesion kinase (FAK). Methods MHCC97-H hepatoma cells were cultured and divided into control group and experimental (sunitinib) group. Experimental groups were added 2.5, 5,10 and 20μmol/L of sunitinib for 24, 48 and 72 hours respectively. The morphological changes were observed before and after sunitinib treatment in MHCC97-H with Giemsa stain. The inhibitory rate of proliferation in MHCC97-H was detected by MTT assay. The expressions of FAK protein before and after sunitinib treatment were detected by Western blot assay. Results Sunitinib showed the inhibitory effect on hepatoma cell line MHCC97-H. Giemsa staining showed that chromatin condensation, nuclear fragmentation, apoptotic bodies and other typical morphological features. The inhibitory rate was the most obvious in 48-h treatment group. The inhibitory rates were (0.433 ± 0.115)%, (32.863 ± 1.471)%, (49.240 ± 2.256)%, (63.797±2.707)%and (58.887±3.409)%for 2.5, 5, 10 and 20μmol/L concentration groups, and there were signifi-cant differences between groups (P<0.05). Results of Western blot assay showed that the expression levels of FAK protein were significantly reduced after different concentrations of sunitinib treatment for 48 h (P<0.05). Conclusion Sunitinib has inhibitory effect on hepatoma cell line MHCC97-H, enhances the apoptosis and decreases the the expression of FAK pro-tein.