Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same
Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.
1. A chemical composition comprising a molecule selected from the group consisting of
wherein the molecule is complexed with a metal or metal ion.
2. The chemical composition according to claim 1 , wherein the metal is selected from the group consisting of 90 Y, Gd, 68 Ga, 57 Co, 60 Co, 52 Fe, 64 Cu and 67 Cu.
3. A bifunctional chelator and targeting moiety conjugate comprising a molecule selected from the group consisting of
wherein the targeting moiety is selected from the group consisting of a peptide and an antibody.
4. The bifunctional chelator and targeting moiety conjugate according to claim 3 , wherein the peptide is selected from the group consisting of a RGD, Asp-Gly-Glu-Ala (DGEA), bombesin peptides (BBN), and uPAR peptides.
5. A method of positron emission tomography (PET) imaging comprising:
introducing into a subject a chemical composition according to claim 2 ; and
imaging the subject after introducing the composition.