Detection of apoptosis by PET/CT with the diethyl ester of [18F]ML-10 and fluorescence imaging with a dansyl analogue |
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| Institution: | 1. Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK;2. Manchester Pharmacy School, University of Manchester, M13 9PT, UK;3. School of Science and Environment, Manchester Metropolitan University, M15 6BH, UK;1. Department of Chemistry, Bar-Ilan University, Ramat-Gan 52900, Israel;2. School of Pharmacy, Institute for Drug Research, The Hebrew University of Jerusalem, Ein Karem, Jerusalem 91120, Israel;3. Faculty of Life Sciences and Institute of Nanotechnology, Bar-Ilan University, Ramat-Gan 52900, Israel;1. Department of Applied Mathematics, University of Colorado, Boulder, CO 80309, United States;2. BioFrontiers Institute, University of Colorado, Boulder, CO 80309, United States;1. Department of Chemistry & Pharmaceutical Sciences, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy;2. Molecular Simulation Engineering (MOSE) Laboratory, DI3, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy;1. Department of Biomedical Sciences, University of Sassari, Sassari, Italy;2. “G. Minardi” Laboratory of Cognitive Neuroscience, Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy |
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| Abstract: | The diethyl ester of 18F]ML-10 is a small molecule apoptotic PET probe for cancer studies. Here we report a novel multi-step synthesis of the diethyl ester of ML-10 in excellent yields via fluorination using Xtal-Fluor-E. In addition, a one-pot radiosynthesis of the diethyl ester of 18F]ML-10 from nucleophilic 18F]fluoride was completed in 23% radiochemical yield (decay corrected). The radiochemical purity of the product was ⩾99%. The diethyl ester of 18F]ML-10 was used in vivo to detect apoptosis in the testes of mice. In parallel studies, the dansyl-ML-10 diethyl ester was prepared and used to detect apoptotic cells in an in vitro cell based assay. |
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| Keywords: | Apoptosis ML-10 PET/CT XtalFluor-E Nucleophilic fluorination Fluorine-18 |
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