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Synthesis and preliminary biodistribution studies of [131I]SIB-PEG4-CHC in tumor-bearing mice

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Abstract

This work reports the synthesis and preliminary biodistribution results of [131I]SIB-PEG4-CHC in tumor-bearing mice. The tributylstannyl precursor ATE-PEG4-CHC was synthesized by conjugation of ATE to amino pegylated colchicine NH2-PEG4-CHC. [131I]SIB-PEG4-CHC was radiosynthesized by electrophilic destannylation of the precursor with a yield of ~44%. The radiochemical purity (RCP) appeared to be >95% by a Sep-Pak cartridge purification. [131I]SIB-PEG4-CHC was lipophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [131I]SIB-PEG4-CHC cleared from background rapidly, and didn’t deiodinate in vivo. However, the poor tumor localization excluded it from further investigations as a tumor-targeted radiopharmaceuticals.

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Acknowledgments

The work was financially supported by National Natural Science Foundation of China (J0630962), the Fundamental Research Funds for the Central Universities (lzujbky-2009-22) and Chunhui Plan (Z2008-1-62018) Sponsored by Ministry of Education, China.

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Authors and Affiliations

  1. Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000, China

    Xiaobei Zheng, Jing Yang, Xiaojiang Duan, Tingting Niu, Wangsuo Wu & Jianjun Wang

  2. Department of Nuclear Medicine, Gansu Academy of Medical Sciences, Lanzhou, 730050, China

    Feng Dong

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  1. Xiaobei Zheng
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  2. Feng Dong
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  3. Jing Yang
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  4. Xiaojiang Duan
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  7. Jianjun Wang
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Correspondence to Jianjun Wang.

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Zheng, X., Dong, F., Yang, J. et al. Synthesis and preliminary biodistribution studies of [131I]SIB-PEG4-CHC in tumor-bearing mice. J Radioanal Nucl Chem 287, 113–117 (2011). https://doi.org/10.1007/s10967-010-0659-5

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  • DOI: https://doi.org/10.1007/s10967-010-0659-5

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