Since angiogenesis is critical to the proliferation of solid tumors, the inhibition of this process may provide a new approach for cancer therapy. TNP-470 (O- (chloroacetyl-carbamoyl) fumagillol), a novel semisynthetic analogue of fumagillin isolated from. Aspergillus fumigatus, has potential as an antiangiogenic agent, which selectively prevents endothelial cell proliferation through inhibition of DNA synthesised. In the present study, the effects of TNP-4700n tumor-induced angiogenesis, tumor proliferation and experimental pulmonary metastasis were examined using a weakly immunogenic squamous cell carcinoma of the WHT/Ht mouse. TNP-470 inhibited the angiogenesis induced by the murine tumor dose-dependently, and the number of blood vessels orientated towards the intradermal tumor was maximally reduced by 45%compared to the control. In the tumor proliferation assay, TNP-470 significantly inhibited proliferation of the subcutaneously inoculated tumor, and reduced the tumor volume by 29% (80㎎/kg) and 46% (40㎎/kg) compared to the control. A similar inhibitory effect on tumor proliferation was observed in the experimental pulmonary metastasis assay, and the number of metastatic foci (diameter≧1.0) after intravenous inoculation of tumor cells was lowered by 13% (80㎎/㎏) and 42% (40㎎/kg) compared to the control with injection of TNP-470. These results suggest that TNP-470 has strong inhibitory activities against in vivo tumor-induced angiogenesis and proliferation of murine squamous cell carcinoma at the subcutaneous and rnetastatic sites.