Copper Cu 64 dotatate is a newly approved Cu labeled somatostatin analog and has several advantages over 68Ga-labeled somatostatin analogs for positron emission tomography (PET). Copper Cu 64 dotatate has a longer half-life and can be produced once a day as opposed to several times a day, and lower positron energy lending to improved spatial resolution. Further studies should be performed to compare the two tracers. Further, PET using Copper Cu 64 dotatate has been found to perform better than the current gold standard of single-photon emission computed tomography (SPECT) using 111In-DTPA-octreotide. In a head-to-head trial, the former tracer detected twice as many lesions as the latter.
CAT No: 10-101-339
CAS No:1426155-87-4
Synonyms/Alias:Copper (64Cu) oxodotreotide; Copper 64-DOTA-tate; Copper Cu-64 dotatate; Copper dotatate Cu-64
Chemical Name:2-[4-[2-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-[[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]-10-(carboxylatomethyl)-7-(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate;copper-64(2+)
Cu-64 DOTA-TATE is a radiolabeled peptide compound that combines the somatostatin analog DOTA-TATE with the positron-emitting radioisotope copper-64. As a member of the radiopharmaceutical family, this conjugate is specifically engineered for advanced molecular imaging and receptor-targeted research. Its structure enables high-affinity binding to somatostatin receptor subtype 2 (SSTR2), a receptor commonly overexpressed in neuroendocrine tumors and various other cell types. The incorporation of copper-64, with its favorable half-life and decay properties, allows for precise tracking and quantification in preclinical and translational studies. Cu-64 DOTA-TATE is valued for its role in elucidating receptor biology, optimizing imaging protocols, and supporting the development of novel diagnostic strategies in oncology and beyond.
Molecular imaging: One of the primary applications of this radiolabeled peptide is in positron emission tomography (PET) imaging studies targeting somatostatin receptors. By leveraging the high specificity of DOTA-TATE for SSTR2 and the positron emission characteristics of copper-64, researchers can visualize and quantify receptor expression in living subjects with exceptional spatial and temporal resolution. This enables the non-invasive assessment of neuroendocrine tumor models, evaluation of receptor density, and monitoring of disease progression or response to experimental interventions in animal studies.
Receptor binding studies: Cu-64 DOTA-TATE is widely used in quantitative in vitro and in vivo receptor binding assays. Its strong affinity for SSTR2 allows for precise determination of receptor occupancy, ligand-receptor kinetics, and binding site density in cellular systems and tissue samples. These studies are essential for characterizing receptor pharmacology, screening novel analogs, and validating new targeting ligands for molecular imaging and targeted delivery applications.
Pharmacokinetic and biodistribution analysis: The radiolabeled nature of this compound enables comprehensive investigation of its pharmacokinetics and biodistribution in preclinical animal models. By tracking the copper-64 signal, researchers can determine tissue uptake, clearance rates, and organ-specific accumulation, providing critical data for optimizing dosing regimens and improving the design of next-generation imaging agents. These insights are instrumental in advancing the understanding of peptide-based radiotracers and refining their application in molecular imaging research.
Radiotracer development: As a prototypical SSTR2-targeted radiotracer, Cu-64 DOTA-TATE serves as a valuable reference compound in the development and benchmarking of new imaging agents. Its well-characterized properties make it an ideal standard for evaluating the performance, stability, and targeting efficacy of novel radiolabeled peptides or small molecules. Comparative studies using this compound support the iterative optimization of tracer chemistry and the identification of candidates with improved imaging characteristics or altered pharmacological profiles.
Radiochemistry and chelation studies: The use of copper-64 in this conjugate provides a robust platform for investigating chelation strategies and radiolabeling techniques. Researchers can explore the stability of DOTA-based chelators under physiological conditions, assess the efficiency of radiolabel incorporation, and study the impact of chelator modifications on biological behavior. These investigations inform the rational design of more effective chelation systems and enhance the reliability of radiolabeled probes for diverse molecular imaging applications.
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