1216897-16-3Relevant academic research and scientific papers
Detection of apoptosis by PET/CT with the diethyl ester of [ 18F]ML-10 and fluorescence imaging with a dansyl analogue
Kadirvel, Manikandan,Fairclough, Michael,Cawthorne, Christopher,Rowling, Emily J.,Babur, Muhammad,McMahon, Adam,Birkket, Paul,Smigova, Alison,Freeman, Sally,Williams, Kaye J.,Brown, Gavin
, p. 341 - 349 (2014)
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.
Microfluidic radiosynthesis and biodistribution of [18F] 2-(5-fluoro-pentyl)-2-methyl malonic acid
Dewkar, Gajanan K.,Sundaresan, Gobalakrishnan,Lamichhane, Narottam,Hirsch, Jerry,Thadigiri, Celina,Collier, Thomas,Hartman, Matthew C. T.,Vaidyanthan, Ganesan,Zweit, Jamal
, p. 289 - 294 (2013/07/28)
Microfluidics technology has emerged as a powerful tool for the radiosynthesis of positron emission tomography (PET) and single-photon emission computed tomography radiolabeled compounds. In this work, we have exploited a continuous flow microfluidic system (Advion, Inc., USA) for the [ 18F]-fluorine radiolabeling of the malonic acid derivative, [ 18F] 2-(5-fluoro-pentyl)-2-methyl malonic acid ([18F]- FPMA), also known as [18F]-ML-10, a radiotracer proposed as a potential apoptosis PET imaging agent. The radiosynthesis was developed using a new tosylated precursor. Radiofluorination was initially optimized by manual synthesis and served as a basis to optimize reaction parameters for the microfluidic radiosynthesis. Under optimized conditions, radio-thin-layer chromatography analysis showed 79% [18F]-fluorine incorporation prior to hydrolysis and purification. Following hydrolysis, the [18F]-FPMA was purified by C18 Sep-Pak, and the final product was analyzed by radio-HPLC (high-performance liquid chromatography). This resulted in a decay-corrected 60% radiochemical yield and ≥98% radiochemical purity. Biodistribution data demonstrated rapid blood clearance with less than 2% of intact [ 18F]-FPMA radioactivity remaining in the circulation 60 min post-injection. Copyright
