Specific modifying agent is coupled to an anti-tumor protein on a certain site. Itconquers the disadvantages which include high antigenicity, short circulating half-life,nonuniform modified sites, inhomogeneous component, reduced activity anduncontrollable quality of the products prepared by non-specific modifying method.The anti-tumor protein coupled with specific modifying agent can be used forthe treatment of tumor and for manufacturing an anti-tumor medicament.