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Preparation and characterization of novel PET molecular probe for detecting tumor apoptosis(PDF)


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Preparation and characterization of novel PET molecular probe for detecting tumor apoptosis
Wang Wei12Lin Jianguo2Liu Guiqing12Qiu Ling12 Lv Gaochao2Li Ke2Luo Shineng12
1.School of Chemical and Materials Engineering,Jiangnan University,Wuxi 214122,China; 2.Key Laboratory of Nuclear Medicine,Ministry of Health and Jiangsu Key Laboratory of Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063,China
positron emission tomagraphy apoptosis imaging probe tumor apoptosis molecular probe peptide DEVD one-step 18F-radiolabeling click chemistry
A novel positron emission tomography(PET)molecular probe is designed and prepared for detecting tumor apoptosis. Its physicochemical and biological properties are evaluated. Precursor 1 is obtained by combining the labeling group with the specific peptide sequence Asp-Glu-Val-Asp(DEVD)using the “click chemistry”. Then,one-step 18F-raidolabeling approach is used to acquire the molecular probe 18F-1. Octanol-water partition coefficient and stability of 18F-1 in PBS and serum are investigated. The results show that 18F-1 is obtained within 40 min in good radiochemical purity(>98%)and high specific activity(1.5 Ci/μmol),and the log P value is -0.995±0.103,indicating its characteristic of hydrophilicity. These results suggest that 18F-1 is a potential PET probe and worthy of further investigation.


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Last Update: 2018-02-28