The invention discloses a PET (
positron emission
tomography)
imaging agent, a precursor and a probe for targeting an EphA2
receptor as well as a preparation method and application of the
PET imaging agent, the precursor and the probe, and a radioactive probe which is formed by labeling a chelating agent (such as
DOTA and NOTA) and a
radionuclide (such as 68Ga) by taking bicyclic
peptide as a targeting group is specifically combined with the EphA2
receptor highly expressed on the surface of a tumor
cell. According to the invention, a conformation limitation strategy is adopted for transforming the
peptide probe targeting EphA2 for the first time, the bicyclic
peptide radioactive probe with excellent targeting performance and in-vivo imaging effect is obtained, the tumor uptake value is high, and tumor and non-
tumor imaging is clear; and successful imaging in a
fibrosarcoma model. According to the EphA2
receptor-targeted
PET imaging agent provided by the invention, the precursor, namely the probe, has the advantages of simplicity in preparation, good targeting property, excellent imaging effect and the like, can be used for
PET imaging diagnosis, prognosis evaluation and
targeted therapy guidance of EphA2 positive tumors, and has good
clinical value.