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Radiolabeling of thioguanine with 125I for diagnosis and therapy: in vitro and in vivo evaluation

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Abstract

Labeling was carried out by direct iodination of thioguanine (100 μg) with radioiodine in a fast single step at 60 °C, to produce iodo-6-thioguanine (125I-S6G). Chloramine-T (200 μg) was used as oxidizing agent to oxidize the iodide ion to the iodonium ion, at pH 7 and the reaction time was 30 min. A high radiochemical yield of 96.4% was obtained. The labeled compound was quantitatively separated and purified by means of high pressure liquid chromatography (HPLC) with a radiochemical purity greater than 98%, which facilitates its clinical use for human application. The biodistribution of 125I-6-thioguanine was studied by injection of the tracer in both normal and tumor bearing mice. The uptake in ascetic fluid was 35.4 and 23.9% at 1 and 24 h post intravenous injection (h.p.i.), respectively, indicating the suitability of this labeled compound for use as a radiopharmaceutical agent.

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Acknowledgements

The authors wish to thank the editor and the referees of the JRNC for their cooperation and valuable comments and also Prof. Dr. K. Farah for her efforts in reviewing the manuscript.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    A. M. Amin

  2. Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    S. E. Soliman

  3. Faculty of Science, Zagazig University, Zagazig, Egypt

    H. M. Killa

  4. Radioisotope Production Project, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    H. A. El-Aziz

Authors
  1. A. M. Amin
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  2. S. E. Soliman
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  3. H. M. Killa
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  4. H. A. El-Aziz
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Correspondence to A. M. Amin.

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Amin, A.M., Soliman, S.E., Killa, H.M. et al. Radiolabeling of thioguanine with 125I for diagnosis and therapy: in vitro and in vivo evaluation. J Radioanal Nucl Chem 283, 273–278 (2010). https://doi.org/10.1007/s10967-009-0349-3

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  • DOI: https://doi.org/10.1007/s10967-009-0349-3

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