Abstract: L-Proline-m-bis (2-chloroethyl) amino-L-phenylalanyl-L-norvaline ethyl ester hydrochloride (MF13) is a new anticancer tripeptide. Our previous study in vitro and in vivo showed that MF13 had anti-proliferative activities in a panel of human hepatocellular carcinoma (HCC) cell lines from different origin. In the present study, we focused on the inhibition effect on HCC of MF13 combined with other anti-cancer drugs. The results of combination chemotherapy in vitro indicated that the combination of MF13 with mitomycin C (MMC) at appropriate concentrations led to a synergistic effect; however, the combination of MF13 with vincristine (VCR) showed no synergistic effect. In the Bel-7402 tumor bearing nude mice, the antitumor effect of the groups of 2 mg·kg^-1 MF13 + 2 mg·kg^-1 MMC or 2 mg·kg^-1 MF13 + 50 mg·kg^-1 cyclophosphamide (CTX) exhibited synergistic anticancer efficacies while the group of 2 mg·kg^-1 MF13 + 0.3 mg·kg^-1 VCR did not have the same effect. Based on our data, we believe that MF13 can be considered as a potential agent against human hepatocellular carcinoma no matter how treated, alone or combined with other drugs.