Mice bearing C666-1tumor grafts were intravenously injected with 100 nmol/kg Z142X, Z142, or an equal amount of control agents or the same volume of PBS every two days for 15 times via tail vein. Tumor growth was monitored by measuring the tumor volume every day. The average tumor sizes increased rapidly in the control groups, while the tumor in the Z142X affitoxin- or Z142 affibody-treated animals displayed remarkable growth inhibition. At the end of the experiment, all tumor grafts were removed and weighed. The average tumor weights in Z142X-treated animals were significantly lower than that in the control mice. Similar to the mice bearing subcutaneously CNE-2Z tumor xenografts, Z142X affitoxin was a much stronger inhibitor than that of control agents. Z142 affibody did exert inhibitory activity to tumor growth. The control agents (ZWTX, PE38KDEL or PBS) did not show anti-tumor effect on these mice. Data represent the mean ± SD (n = 5). *P<0.05, compare to the PBS, PE38KDEL, ZWTX, Z142 affibody groups. 2-tailed unpaired Student’s t test was used.