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

摘要

The aim of this study was to develop a radiopharmaceutical for the imaging of CXCR4-expressing tumors in vivo. For ~(125)I-labeling, ~(125)I-SIB was synthesized and conjugated with the ε-NH _2 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 ~(125)I-IB-Ac-TZ14011 was mainly excreted via the kidney, and further evaluation in mice with induced tumors was necessary.