化药新药研发其他>方法开发检测 | 使用Biotage Isolera快速纯化液相制备色谱进行一个新型的18F人工基团的合成by耐士科技-上海鑫欣生物科技有限公司

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应用领域	制药/生物制药
检测样本	化药新药研发
检测项目	其他>方法开发
参考标准	GB/T 8****

The [18F]fluorocyclobutyl group has the potential to be a metabolically stable prosthetic group for PET tracers. The synthesis of the radiolabeling precursor cis-cyclobutane-1,3-diyl bis(toluene-4-sulfonate) 8 was obtained from epibromohydrin in 7 steps (2% overall yield). The radiolabeling of this precursor 8 and its conjugation to L-tyrosine as a model system was successfully achieved to give the new nonnatural amino acid 3-[18F]fluorocyclobutyl-L-tyrosine (L-3-[18F]FCBT) [18F]17 in 8% decay-corrected yield from the non-carrier-added [18F]fluoride. L-3-[18F]FCBT was investigated in vitro in different cancer cell lines to determine the uptake and stability. The tracer [18F]17 showed a time dependent uptake into different tumor cell lines (A549, NCI-H460, DU145) with the best uptake of 5.8% injected dose per 5 105 cells after 30 min in human lung carcinoma cells A549. The stability of L-3-[18F]FCBT in human and rat plasma and the stability of the non-radioactive L-3-FCBT in rat hepatocytes were both found to be excellent. These results show that the non-natural amino acid L-3-[18F]FCBT is a promising metabolically stable radiotracer for positron emission tomography.

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上一篇耐士科技：使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技

下一篇使用Biotage Isolera快速纯化液相制备色谱为设计新的抗结核药物探索解旋酶ATPase结构 by Biotage Isolera耐士科技

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