In recent years, the potential anti-cancer mechanisms of ginsenoside Rg3 have been demonstrated in various cancer models, which include the inhibition of cell proliferation and induction of apoptosis via down-regulating PI3K/Akt, and activation of caspase-3 and -9 and Bcl-2 family proteins [234, 252], induction of cell cycle arrest by regulating CDK pathway [240], inhibition of metastasis through reducing the expressions of aquaporin 1, C–X–C chemokine receptor type 4 (CXCR4) and hypoxia-inducible factor 1α (HIF-1α) [253–255]. This evidence concerns the gene CXCR4 and cancer.