Brand-new skeleton 99MTC-FAPI diagnostic probe and use thereof in preparation of drug or reagent for diagnosing tumors
The present disclosure discloses a brand-new skeleton 99mTc-FAPI diagnostic probe and use thereof in the preparation of a drug or a reagent for diagnosing tumors, wherein the structural formula of a dimeric compound targeting FAP is shown by following formula. Compared with conventional FAP inhibitor radiopharmaceuticals, technetium-99m-labeled novel skeleton FAP inhibitor dimeric compound has a very high tumor uptake rate, high contrast between tumor and background and good in vivo biodistribution.
1 . A dimeric compound targeting FAP or a pharmaceutically acceptable salt thereof, wherein the dimeric compound targeting FAP has a structure as follows:
wherein R 1 is selected from cyano;
R 2 is selected from hydrogen, fluoro or chloro;
R 3 is selected from hydrogen or methyl;
R 4 is selected from hydrogen, methyl, ethyl, propyl, cyclopropyl or cyclobutyl;
R 5 and R 6 are independently selected from hydrogen, methyl, fluoro or chloro;
R 7 and R 8 are independently selected from hydrogen or methyl;
L 1 and L 2 are independently selected from any one of:
Y is selected from any one of:
Q is a hydrogen atom or is used as a nuclide chelating group moiety, and is selected from any one of:
2 . A dimeric compound targeting FAP and a pharmaceutically acceptable salt thereof, wherein the dimeric compound is selected from any one of:
3 . The dimeric compound targeting FAP or pharmaceutically acceptable salt thereof according to claim 1 , wherein the pharmaceutically acceptable salt is selected from the group consisting of hydrochlorides, sulfates, trifluoroacetates, fumarates, succinates, sulfonates, maleates, acetates, phosphates and citrates.
4 . A radionuclide technetium-99m labelled compound targeting fibroblast activation protein, wherein the radionuclide technetium-99m labelled compound targeting fibroblast activation protein is prepared through reaction of the dimeric compound targeting FAP or pharmaceutically acceptable salt thereof according to claim 1 with a compound containing radionuclide technetium-99m according to an existing wet labeling method or a freeze-drying labeling method.
5 . A 99m-Tc labelled kit, comprising the dimeric compound targeting FAP or pharmaceutically acceptable salt thereof according to claim 1 , a ligand forming coordination with technetium-99m, a reductant, an additive, and a stabilizer.