Abstract: Objective To investigate the inhibitory effect of XK469 on the in vitro growth of H460 cells and its mechanism. Methods The survival curves of H460 cells treated with XK469, XN472 and adriamycin, respectively, were obtained by MTT analysis, and the effect of XK469 and adriamycin on the cell cycle of H460 cells examined by flow cytometry. Western blotting was adopted for detecting the expression of cdc2 and phos-cdc2 induced by XK469 and adriamycin. Results Different concentrations of XK469 and adriamycin could significantly inhibit the growth of H460 cells, induce their G2/M phase arrest, and increase phos-cdc2 expression; XN472 had a lesser effect on the growth of H460 cells. Conclusion XK469 can increase phos-cdc2 expression and induce G2/M phase cell cycle arrest of H460 cells, resulting in inhibition of H460 cell growth. The inhibitory effect of XK469 on H460 cell growth is attributed to the chlorine in the 7-positon of its structure.