David, Tomas published the artcileImproved Conjugation, 64-Cu Radiolabeling, in Vivo Stability, and Imaging Using Nonprotected Bifunctional Macrocyclic Ligands: Bis(Phosphinate) Cyclam (BPC) Chelators, Application In Synthesis of 1353016-70-2, the publication is Journal of Medicinal Chemistry (2018), 61(19), 8774-8796, database is CAplus and MEDLINE.
Bifunctional derivatives of Bis(Phosphinate)-bearing Cyclam (BPC) chelators bearing carboxylate, amine, isothiocyanate, azide or cyclooctyne in BP-side chain were synthesized. Conjugations required no protection of phosphinate or ring secondary amine groups. The ring amines were not reactive (proton protected) at pH < ∼8. For isothiocyanate coupling, oligopeptide N-terminal α-amines were more suitable than alkyl amines, e.g. Lys ω-amine (pKa ∼7.5-8.5 and ∼10-11, resp.) due to lower basicity. The Cu-64 labeling was efficient at room temperature (specific activity ∼100 GBq/μmol; 25°C, pH 6.2, ∼100 ligand equivalent, 10 min). A representative Cu-64-BPC was tested in-vivo showing fast clearance and no non-specific radioactivity deposition. The monoclonal anti-PSCA antibody 7F5 conjugates with thiocyanate BPC derivative or NODAGA were radiolabeled and studied in PC-3-PSCA tumor bearing mice by PET. The radiolabeled BPC conjugate was accumulated in the prostate tumor with low off-target uptake, unlike Cu-64-labeled NODAGA-antibody conjugate. The BPC chelators have a great potential for theranostic applications of Cu-64/Cu-67 matched pair.
Journal of Medicinal Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Application In Synthesis of 1353016-70-2.
Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider