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Kit-like 18F-labeling of an estradiol derivative as a potential PET imaging agent for estrogen receptor-positive breast cancer

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Abstract

16α-18F-fluoroestradiol (18F-FES) has been developed as a promising positron emission tomography (PET) imaging agent for targeting estrogen receptor positive (ER+) breast cancer in the clinical trial. However, the radiosynthesis of 18F-FES often requires two steps and tough experimental conditions. Therefore, a new estradiol derivative (18F-AmBF3-ES) was prepared by an efficient one-step 18F-radiolabeling method. The tracer was obtained in high yield (~65%) and excellent radiochemical purity (>98%) within 30 min. The uptake rate of 18F-AmBF3-ES in ER+ cells was about 3.5% at 30 min. The results suggested that the tracer may be a potential PET imaging agent for ER+ breast cancer.

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Acknowledgements

This work was financially supported by Natural Science Foundation of China (21371082), Natural Science Foundation of Jiangsu Province (BK20141102 and BK20151118) and Key Medical Talent Project of Jiangsu Province (RC2011097).

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Authors and Affiliations

  1. School of Chemical and Materials Engineering, Jiangnan University, Wuxi, 214122, People’s Republic of China

    Guiqing Liu, Wei Wang, Xueyu Zhao, Shanshan Wang, Shineng Luo & Ling Qiu

  2. Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, 214063, People’s Republic of China

    Guiqing Liu, Wei Wang, Jianguo Lin, Ke Li, Gaochao Lv, Xueyu Zhao, Shanshan Wang, Shineng Luo & Ling Qiu

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  1. Guiqing Liu
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  2. Wei Wang
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  4. Ke Li
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Correspondence to Jianguo Lin or Ling Qiu.

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Liu, G., Wang, W., Lin, J. et al. Kit-like 18F-labeling of an estradiol derivative as a potential PET imaging agent for estrogen receptor-positive breast cancer. J Radioanal Nucl Chem 312, 599–607 (2017). https://doi.org/10.1007/s10967-017-5245-7

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  • DOI: https://doi.org/10.1007/s10967-017-5245-7

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