Abstract: Conjugate of biomacromolecule with bioreductive which can be useful for treating tumor is provided. The biomacromolecule is selected from apo-transferrin, Fe-transferrin, Ru-transferrin, Ti-transferrin, Ga-transferrin, Pt-transferrin, somatostatin, EGF, folacin acid or transcobalamin, and the bioreductive agent is selected from quinones, aromatic nitrogen oxides, fatty nitrogen oxides, heterocyclic nitro compound, transition metal compound. Such conjugate can selectively target the tumor cells, and lower the toxicity of medicines and survivability of tumor cells, so that the conjugate can be used for delivery of anti-tumor compounds or treating tumors.