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Synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine and its biological evaluation in B16 melanoma-bearing mice as PET tracer for tumor imaging

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Abstract

O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET), a fluorine-18 labeled analogue of tyrosine, has been synthesized and biologically evaluated in tumor-bearing mice. The whole synthesis procedure is completed within 50 min. The radiochemical yield is about 40% (no decay corrected) and radiochemical purity more than 97% after simplified solid phase extraction. [18F]FET shows rapid, high uptake and long retention in the tumor as well as low uptake in the brain. The ratios of tumor-to-muscle (T/M) and tumor-to-blood (T/B) of [18F]FET are similar to those of [18F]FDG, but the ratios of tumor-to-brain (T/Br) are 2–3 times higher than that of [18F]FDG. Autoradiography of [18F]FET demonstrates a remarkable accumulation in melanoma with high contrast. It appears to be a probable competitive candidate for melanoma imaging with PET.

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Authors and Affiliations

  1. Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, 201800, China

    Wang MingWei, Yin DuanZhi, Li ShiQiang & Wang YongXian

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  1. Wang MingWei
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  2. Yin DuanZhi
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  3. Li ShiQiang
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  4. Wang YongXian
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Correspondence to Yin DuanZhi.

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Supported by the Knowledge Innovation Project of Chinese Academy of Sciences (No. KJCX1-SW-08) and the National Natural Science Foundation of China (Grant No. 30371634)

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Wang, M., Yin, D., Li, S. et al. Synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine and its biological evaluation in B16 melanoma-bearing mice as PET tracer for tumor imaging. SCI CHINA SER B 50, 276–283 (2007). https://doi.org/10.1007/s11426-007-0023-y

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