The anti-tumor agent, (Z)-3-(chloromethylene)-6-chlorothiochroman-4-one, could inhibit tumor cell proliferations. However, the anti-tumor activity in vivo is poorly understood. So we research the anti-tumor activity in vitro and in vivo, and the probable anti-tumor mechanism systematically in this study. The results showed that the compound CMCT was effective with tumor as the concentration-dependent in vitro and in vivo, and the toxicology of CMCT affecting body weight, WBC, organ and bone in mice was lower than DDP. It would be specially mentioned that ILS of the S180 ascites tumor models was 90.22% at the dose of 10 mg/ (kg·d) by peritoneal injection; In addition, the result showed that CMCT could induce cell thapoptosis and inhibit tubulin aggregation to play an efficient role against tumor. All in all, The compound of CMCT which possessed obvious anti-tumor activity and lower toxicity deserved further research on its anti-tumor mechanism deeply.