1374994-87-2

Upstream product

• 174137-97-4 1,4-bis(tert-butoxycarbonylmethyl)-1,4,7-triazacyclononane 
• 100-11-8 1-bromomethyl-4-nitro-benzene 

Downstream Products

• 1310363-31-5 4,7-bis(carboxymethyl)-1-(4-amino-benzyl)-1,4,7-triazacyclononane 
• 1374994-81-6 (2,2′-(7-(4-isothiocyanatobenzyl)-1,4,7-triazonane-1,4-diyl)diacetic acid) 
• 1402034-42-7 C₄₅H₆₅N₁₃O₁₂S 

Relevant academic research and scientific papers

IMPROVED METHODS OF IMAGING WITH Ga-68 LABELED MOLECULES

The present application discloses compositions and methods of use of 68Ga labeled molecules. Preferably, the 68Ga is attached to a peptide targetable construct and is used in a pretargeting technique with a bispecific antibody (bsAb). The bsAb comprises at least one binding site for a disease-associated antigen, such as a tumor-associated antigen, and at least one binding site for a hapten on the targetable construct. Exemplary haptens include In-DTPA and HSG. More preferably, the bsAb is administered about 24-30 hours before the targetable construct, and detection by PET imaging occurs about 1-2 hours after the targetable construct is administered. The methods and compositions are suitable for detection, diagnosis and/or imaging of various diseases, such as cancer or infectious disease.

TRIAZANONANE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR ENHANCED FLUORINE-18 LABELING

The present invention relates to a triazanonane derivative indicated by the chemical formula 1 below, or a pharmaceutically acceptable salt thereof, and a method for preparing same, and the triazanonane derivative according to the present invention forms a complex with a metal-fluoride and displays an effect of increasing the labeling efficiency up to 78-90% when labeling F-18, thus enabling use in various radioactive medicine labeling (In the chemical formula 1, R1, R2, A. E. X, n and m are as defined in the present description.)

Development of a bifunctional chelating agent containing isothiocyanate residue for one step F-18 labeling of peptides and application for RGD labeling

We report herein a novel isothiocyanate active ligand for fluorine-18 labeling prepared by four step synthesis. It can be conjugated to a target molecule containing an amino functional group under weak basic conditions by way of thiourea bond formation. We explored the application of synthesized ligand by conjugating to well known αvβ3 integrin targeting peptide, c(RGDyK). The conjugated peptide showed good radiochemical yield and efficiency with an excellent radiochemical purity (97.1 ± 1.2%) in a short reaction time (10 min). Labeled peptide showed excellent in vitro and in vivo stability (>95%). αvβ3 integrin specific tumor uptake was observed both in biodistribution and small animal microPET studies on αvβ3-positive U87MG (human glioma cells) xenograft bearing mice. In general, successful application of synthesized ligand for labeling of RGD peptide could facilitate the possibility of using this ligand for labeling peptides containing an amino functional group.