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Synthesis and biological studies of 99mTc(HYNIC–MFL)(tricine)(TPPTS) as a novel tumor imaging agent

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Abstract

This work reports the synthesis, radiolabeling and biological studies of 99mTc(HYNIC–MFL)(tricine)(TPPTS) in tumor-bearing mice. The novel melphalan derivative was successfully synthesized by conjugation of HYNIC to melphalan. The ligand could be labeled by 99mTc in high yield to get 99mTc(HYNIC–MFL)(tricine)(TPPTS), which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that 99mTc(HYNIC–MFL)(tricine)(TPPTS) accumulated in the tumor with favorable uptake and retention. The good accumulation in tumor tissue, high tumor/muscle ratios and satisfactory scintigraphic images highlight the potential of 99mTc(HYNIC–MFL)(tricine)(TPPTS) for tumor imaging.

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Acknowledgments

The work was financially supported by National Key Basic Research Program of China (2013CB932703) and National Natural Science Foundation of China (11575211, 21371172, 11475198, 21401198).

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Authors and Affiliations

  1. Key Laboratory of Nuclear Radiation and Nuclear Energy Technology, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing, 100049, China

    J. Wang, W. Yang, J. Xue, Y. Zhang, W. Han & Y. Liu

  2. Beijing Engineering Research Center of Radiographic Techniques and Equipment, Beijing, 100049, China

    J. Wang, W. Yang, J. Xue, Y. Zhang, W. Han & Y. Liu

Authors
  1. J. Wang
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  2. W. Yang
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  3. J. Xue
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  4. Y. Zhang
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  5. W. Han
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  6. Y. Liu
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Correspondence to J. Wang or Y. Liu.

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Wang, J., Yang, W., Xue, J. et al. Synthesis and biological studies of 99mTc(HYNIC–MFL)(tricine)(TPPTS) as a novel tumor imaging agent. J Radioanal Nucl Chem 310, 1209–1213 (2016). https://doi.org/10.1007/s10967-016-4955-6

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  • DOI: https://doi.org/10.1007/s10967-016-4955-6

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