This study is to investigate the anticancer effects and mechanisms of Tegillarca granosa Linnaeus-1 (TG-1) on renal carcinoma OS-RC-2 cells in vitro. The proliferation of OS-RC-2 cells was evaluated under various concentrations of TG-1 using MTT assay. The apoptosis of OS-RC-2 cells was analyzed using acridine orange/ethidium bromide staining. And the cell cycle distribution of OS-RC-2 cells was detected by flow cytometry. In addition, the expression level of Ki67 mRNA was examined by RT-PCR and level of casepase-3 was examined by Western blot analysis. TG-1 incubation significantly inhibited the proliferation of renal carcinoma OS-RC-2 cells and arrested cells at G0/G1 phase (P <0.05). And TG-1 also significantly inhibited the expression of Ki67 mRNA (P<0.05). Additionally, TG-1 significantly promoted apoptosis and the expression of caspase-3 in cells (P<0.05). Moreover, the optimal effects of TG-1 was achieved at the concentration of 100 mg/L The results indicate that TG-1 has antitumor effects on renal carcinoma OS-RC-2 cells and that the underlying mechanisms may be acted through inhibiting proliferation and Ki67 mRNA expression, and promoting apoptosis and caspase-3 expression.