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Synthesis and preliminary evaluation of a novel 125I-labeled T140 analog for quantitation of CXCR4 expression |
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| Authors: | Yanjiang Han Duanzhi Yin Mingqiang Zheng Wei Zhou ZhenHong Lee Lan Zhan Yufei Ma Mingxing Wu Lingli Shi Ni Wang Jianbo Lee Cheng Wang Zheng Lee Yongxian Wang |
| Institution: | 1. Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, China 2. Graduate School, Chinese Academy of Sciences, Beijing, China 3. Department of Nuclear Medicine/Radiology, University Hospitals Case Medical Center, Case Western Reserve University, Cleveland, OH, USA |
| Abstract: | The aim of this study was to develop a radiopharmaceutical for the imaging of CXCR4-expressing tumors in vivo. For 125I-labeling, 125I-SIB was synthesized and conjugated with the ε-NH2 group of Ac-TZ14011, a specific CXCR4 antagonist. The specific radioactivity of the product was 5 GBq/μmol and the radiochemical purity (RCP) was 96% (n = 3). After 6 h, the RCP of the product in PBS was 93%. The MCF-7 cell uptake of Ac-TZ14011 was rapid and high. Primary biodistribution studies indicated that 125I-IB-Ac-TZ14011 was mainly excreted via the kidney, and further evaluation in mice with induced tumors was necessary. |
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