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Kit-like 18F-labeling of an estradiol derivative as a potential PET imaging agent for estrogen receptor-positive breast cancer

Journal 2017 · IF 1.282 · 312(3): 599-607 · 发表于 2017 年 4 月 13 日
作者: Liu Guiqing,Wang Wei,Lin Jianguo,Li Ke,Lv Gaochao,Zhao Xueyu,Wang Shanshan,Luo Shineng,Qiu Ling
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摘要

16α- 18 F-fluoroestradiol ( 18 F-FES) has been developed as a promising positron emission tomography (PET) imaging agent for targeting estrogen receptor positive (ER + ) breast cancer in the clinical trial. However, the radiosynthesis of 18 F-FES often requires two steps and tough experimental conditions. Therefore, a new estradiol derivative ( 18 F-AmBF 3 -ES) was prepared by an efficient one-step 18 F-radiolabeling method. The tracer was obtained in high yield (~65%) and excellent radiochemical purity (>98%) within 30 min. The uptake rate of 18 F-AmBF 3 -ES in ER + cells was about 3.5% at 30 min. The results suggested that the tracer may be a potential PET imaging agent for ER + breast cancer.