{0><}0{>The invention discloses a radio-labeled tumor developing agent as well as a preparation method and application thereof. <0}{0><}0{>The radio-labeled tumor developing agent structurally contains an alpha-amino acid derivate structure capable of labeling nuclide and a tumor-targeted folic acid molecule, wherein radionuclide is 18F, and the alpha-amino acid derivate structure and the folic acid molecule are connected in a specific chemical mode. <0}{0><}0{>The invention further relates to a preparation method of the compound and application of the compound serving as a tracing developing agent in PET development in a human body or an animal body. The radio-labeled tumor developing agent has the advantages of simplicity in preparation, low price and strong targeting property especially when serving as a tumor developing agent.