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.

引用

页码：279 / 286

页数：7

共 50 条

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