A combination of INK128 and CDDP is significantly more effective than either single agent in suppressing the growth of NSCLC xenografts (A and B) without enhancing toxicity (A) in nude mice. H460 xenografts were treated with the vehicle control, INK128 (0.5 mg/kg administered by oral gavage daily), CDDP (2 mg/kg administered intraperitoneally once every 3 days), or a combination of INK and CDDP starting on the same day after grouping. Tumor sizes (A, upper panel) and mouse body weights (A, lower panel) were measured every 2 days as indicated. The data presented are mean values ± standard errors. After 22 days, the mice were sacrificed and the tumors were removed and weighed (B). *, P < 0.05; **, P < 0.01; ***, P < 0.001; ****, P < 0.0001 (compared with the vehicle-treated control).