FAPI-2286

FAPI-2286/FAP-2286/CasNo:2581741-18-4 is a potent and selective FAP-binding peptide coupled to a radionuclide chelator with a mean IC50 value of 2.7 nM for binding to FAP. FAP-2286 consists of two functional elements: a FAP-targeting peptide and a chelator used to attach radioisotopes. FAP-2286 and its metal complexes demonstrated high affinity to FAP recombinant protein and cell surface FAP expressed on fibroblasts. Biodistribution studies in mice showed rapid and persistent uptake of 68Ga-FAP-2286, 111In-FAP-2286, and 177Lu-FAP-2286 in FAP-positive tumors, with renal clearance and minimal uptake in normal tissues. 177Lu-FAP-2286 exhibited antitumor activity in FAP-expressing HEK293 tumors and sarcoma patient-derived xenografts, with no significant weight loss. In addition, FAP-2286 maintained longer tumor retention and suppression in comparison to FAPI-46.

msds of FAPI-2286