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Synthesis of 131 I-Labeled-[ 131 I]Iodo-17-Allylamino-17-Demethoxy Geldanamycin ([ 131 I]Iodo-17-AAG) and Its Biodistribution in Mice

2007; Mary Ann Liebert, Inc.; Volume: 22; Issue: 5 Linguagem: Inglês

10.1089/cbr.2006.363

1557-8852

Chen Daozhen, Lu Liu, Min Yang, Xinyu Jiang, Ying Huang,

Cancer, Hypoxia, and Metabolism

Aim: The aim of this study was to examine the radioiodinating condition of 17-allylamino-17-demethoxy geldanamycin (17-AAG) and observe its biodistribution in the hepatoma cell line HepA tumorearing ICR mice for understanding the possibility of its application in nuclear medicine. Methods: [131I]Iodo-17-AAG was prepared by the reaction of 17-AAG with Na[131I] in the presence of hydrogen peroxide. [131I]Iodo-17-AAG was purified by high-performance liquid chromatography (HPLC). The stability of [131I]Iodo-17-AAG was measured by thin-layer chromatography (TLC). The distributions in HepA tumor-bearing ICR mice at 0.5, 1, 4, 8, 24, and 48 hours after injection of [131I]Iodo-17-AAG were measured. Tumor uptake studies were performed in HepA tumor-bearing ICR mice. Results: The labeling yield was over 83%. The radiochemical purity of [131I]Iodo-17-AAG was 99.6% after purification. The specific activity was greater than 4 Ci/μmol. The labeled compound was stable for at least 120 hours in saline at 4°C. It was initially in blood at 5 minutes with 4.79% of injected dose per g of tissue (%ID/g), and then dropped 0.33% ID/g at 24 hours. The uptake in liver, lung, and kidney at 4.44% ID/g, 2.03% ID/g, and 2.17% ID/g decreased with time, and less than 1% ID/g was measured after 24 hours in those organs. There was rapid tumor uptake, which reached 1.26% ID/g at 0.5 hours, the highest uptake at 8 hours. Yet, the [131I]Iodo-17-AAG in the contralateral muscle was at a low level during the 48 hours. The tumor-contralateral muscle (T/CM) radioactivity ratio for [131I]Iodo-17-AAG remained constant at all time points. Conclusions: [131I]Iodo-17-AAG can be efficiently radiolabeled at high specific activity, purified by HPLC and stored with little radiolysis at this specific activities. [131I]Iodo-17-AAG is a promising radiopharmaceutical in nuclear medicine, especially for tumor-targeted radionuclide brachytherapy.