1400993-41-0Relevant academic research and scientific papers
Methods and compositions for the rapid synthesis of radiometal-labeled probes
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Page/Page column 16; 17; 18; 19, (2016/10/17)
The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.
Strain-promoted catalyst-free click chemistry for rapid construction of 64Cu-labeled PET imaging probes
Chen, Kai,Wang, Xinlu,Lin, Wei-Yu,Shen, Clifton K.-F.,Yap, Li-Peng,Hughes, Lindsey D.,Conti, Peter S.
supporting information, p. 1019 - 1023 (2013/02/22)
A rapid, efficient, and catalyst-free click chemistry method for the construction of 64Cu-labeled PET imaging probes was reported based on the strain-promoted aza-dibenzocyclooctyne ligation. This new method was exemplified in the synthesis of 64Cu-labeled RGD peptide for PET imaging of tumor integrin αvβ3 expression in vivo. The catalyst-free click chemistry reaction proceeded with a fast rate and eliminated the contamination problem of the catalyst Cu(I) ions interfering with the 64Cu radiolabeling procedure under the conventional Cu-catalyzed 1,3-dipolar cycloaddition condition. The new strategy is simple and robust, and the resultant 64Cu-labeled RGD probe was obtained in an excellent yield and high specific activity. PET imaging and biodistribution studies revealed significant, specific uptake of the click 64Cu-labeled RGD probe in integrin αvβ 3-positive U87MG xenografts with little uptake in nontarget tissues. This new approach is versatile, which warrants a wide range of applications for highly diverse radiometalated bioconjugates for radioimaging and radiotherapy.
