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• W2080771324 endingPage "1782" @default.
• W2080771324 startingPage "1775" @default.
• W2080771324 abstract "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 (<2.2%), and high tumor-to-blood ratio (6.4) at 120 h. 3p-C-NETA possesses favorable in vitro and in vivo profiles and is an excellent bifunctional chelator that can be used for targeted RIT applications using 90Y and 177Lu and has the potential to replace DOTA and DTPA analogues in current clinical use." @default.
• W2080771324 created "2016-06-24" @default.
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• W2080771324 date "2012-08-10" @default.
• W2080771324 modified "2023-09-24" @default.
• W2080771324 title "Synthesis and Preclinical Evaluation of Bifunctional Ligands for Improved Chelation Chemistry of ⁹⁰Y and ¹⁷⁷Lu for Targeted Radioimmunotherapy" @default.
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• W2080771324 doi "https://doi.org/10.1021/bc200696b" @default.
• W2080771324 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3447103" @default.
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