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Title: Fluorine-18 radiolabeling of a nitrophenyl sulfoxide and its evaluation in an SK-RC-52 model of tumor hypoxia
Austin Authors: Laurens, Evelyn;Yeoh, Shin Dee;Rigopoulos, Angela;O'Keefe, Graeme J;Tochon-Danguy, Henri J ;Chong, Lee Wenn;White, Jonathan M;Scott, Andrew M ;Ackermann, Uwe 
Affiliation: School of Chemistry, The University of Melbourne, Melbourne, Victoria, Australia
Bio21 Institute, The University of Melbourne, Melbourne, Victoria, Australia
Department of Molecular Imaging and Therapy, Austin Health, Heidelberg, Victoria, Australia
Olivia Newton-John Cancer Research Institute, Heidelberg, Victoria, Australia
Faculty of Medicine, Dentistry and Health Sciences, The University of Melbourne, Melbourne, Victoria, Australia
School of Cancer Medicine, La Trobe University, Bundoora, Victoria, Australia
Issue Date: Aug-2016
Date: 2016-07-19
Publication information: Journal of Labelled Compounds and Radiopharmaceuticals 2016; 59(10): 416-423
Abstract: The significance of imaging hypoxia with the positron emission tomography ligand [18 F]FMISO has been demonstrated in a variety of cancers. However, the slow kinetics of [18 F]FMISO require a 2-h delay between tracer administration and patient scanning. Labeled chloroethyl sulfoxides have shown faster kinetics and higher contrast than [18 F]FMISO in a rat model of ischemic stroke. However, these nitrogen mustard analogues are unsuitable for routine production and use in humans. Here, we report on the synthesis and in vitro and in vivo evaluation of a novel sulfoxide, which contains an ester moiety for hydrolysis and subsequent trapping in hypoxic cells. Non-decay corrected yields of radioactivity were 1.18 ± 0.24% (n = 27, 2.5 ± 0.5% decay corrected radiochemical yield) based on K[18 F]F. The radiotracer did not show any defluorination and did not undergo metabolism in an in vitro assay using S9 liver fractions. Imaging studies using an SK-RC-52 tumor model in BALB/c nude mice have revealed that [18 F]1 is retained in hypoxic tumors and has similar hypoxia selectivity to [18 F]FMISO. Because of a three times faster clearance rate than [18 F]FMISO from normoxic tissue, [18 F]1 has emerged as a promising new radiotracer for hypoxia imaging.
DOI: 10.1002/jlcr.3426
Journal: Journal of Labelled Compounds and Radiopharmaceuticals
PubMed URL:
Type: Journal Article
Subjects: SK-RC-52 tumor model
Small animal imaging
Appears in Collections:Journal articles

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