Synthesis and preliminary evaluation of a novel ¹²⁵I-labeled T140 analog for quantitation of CXCR4 expression

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• 作者：Yanjiang Han ; Duanzhi Yin ; Mingqiang Zheng ; Wei Zhou ; ZhenHong Lee ; Lan Zhan ; Yufei Ma ; Mingxing Wu ; Lingli Shi and Ni Wang ; et al.
• 关键词：CXCR4 ; SDF ; 1 ; SIB ; Radioiodination
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2010
• 出版时间：May, 2010
• 年：2010
• 卷：284
• 期：2
• 页码：279-286
• 全文大小：331.4 KB

文摘

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.