1392222-50-2

Upstream product

• 1142811-83-3 {tert-butoxycarbonylmethyl-[1-hydroxymethyl-4-(4-nitrophenyl)butyl]amino}acetic acid tert-butyl ester 
• 1258945-71-9 di-tert-butyl 2,2'-(2-bromo-5-(4-nitrophenyl)pentylazanediyl)diacetate 
• 1392222-48-8 tert-butyl 2-{[2-(tert-butoxy)-2-oxoethyl][2-iodo-5-(4-nitrophenyl)pentyl]amino}acetate 
• 1258946-46-1 tert-butyl 2-[(1-{4,7-bis[2-(tert-butoxy)-2-oxoethyl]-1,4,7-triazonan-1-yl}-5-[4-nitrophenyl]pentan-2-yl)[2-(tert-butoxy)-2-oxoethyl]amino]acetate 

Downstream Products

• 1392222-51-3 {4-[5-(4-amino-phenyl)-2-bis(carboxymethyl)aminopentyl]-7-carboxymethyl-[1,4,7]triazo-nan-1-yl}acetic acid 

Relevant academic research and scientific papers

Synthesis and preclinical evaluation of bifunctional ligands for improved chelation chemistry of 90Y and 177Lu for targeted radioimmunotherapy

We report a practical and high-yield synthesis of a bimodal bifunctional ligand 3p-C-NETA-NCS containing the isothiocyanate group for conjugation to a tumor targeting antibody. 3p-C-NETA-NCS was conjugated to a tumor-targeting antibody, trastuzumab, and the corresponding 3p-C-NETA-trastuzumab conjugate was evaluated and compared to trastuzumab conjugates of the known bifunctional ligands C-DOTA, C-DTPA, and 3p-C-DEPA for radiolabeling kinetics with 90Y and 177Lu. 3p-C-NETA-trastuzumab conjugate exhibited extremely rapid complexation kinetics with 90Y and 177Lu. 90Y-3p-C-NETA-trastuzumab and 177Lu-3p-C-NETA-trastuzumab conjugates were stable in human serum for 2 weeks. A pilot biodistribution study was conducted to evaluate in vivo stability and tumor targeting of 177Lu-radiolabeled trastuzumab conjugate using nude mice bearing ZR-75-1 human breast cancer. 177Lu-3p-C-NETA-trastuzumab conjugate displayed low radioactivity level at blood (1.6%), low organ uptake (90Y and 177Lu and has the potential to replace DOTA and DTPA analogues in current clinical use.