In this study, we reported for the first time that fluspirilene is a potential CDK2 inhibitor, and demonstrated for the first time that oral administration of fluspirilene (15 mg/kg) exhibited significant and strong anti-cancer efficacy comparable to the leading cancer drug 5-fluorouracil (10 mg/kg) in vivo in nude mice xenografted with hepatoma Huh7 cells. Here, CDK2 is linked to hepatocellular carcinoma.