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

被引：0
|
作者：
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
机构：
[1] Chinese Academy of Sciences,Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics
[2] Chinese Academy of Sciences,Graduate School
[3] Case Western Reserve University,Department of Nuclear Medicine/Radiology, University Hospitals Case Medical Center
来源：
Journal of Radioanalytical and Nuclear Chemistry | 2010年 / 284卷
关键词：
CXCR4; SDF-1; SIB; Radioiodination;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
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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页码：279 / 286
页数：7
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