FAPI-mFS is a selective fibroblast activation protein ( FAP ) inhibitor with an IC 50 of 0.0014 μM against human FAP . Through its covalent binding property with FAP , FAPI-mFS enhances its uptake and retention time in cancer cells. When radiolabeled with 68 Ga, FAPI-mFS serves as a PET/CT imaging agent with superior tumor-to-background tissue contrast and lesion detection capability. When radiolabeled with 177 Lu or 225 Ac, FAPI-mFS induces tumor regression and inhibition in preclinical models. FAPI-mFS can be used in studies related to cancer and radionuclide-conjugated drugs (RDC).
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