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dc.contributor.authorLaurens, Evelyn-
dc.contributor.authorYeoh, Shin Dee-
dc.contributor.authorRigopoulos, Angela-
dc.contributor.authorO'Keefe, Graeme J-
dc.contributor.authorTochon-Danguy, Henri J-
dc.contributor.authorChong, Lee Wenn-
dc.contributor.authorWhite, Jonathan M-
dc.contributor.authorScott, Andrew M-
dc.contributor.authorAckermann, Uwe-
dc.identifier.citationJournal of Labelled Compounds and Radiopharmaceuticals 2016; 59(10): 416-423en_US
dc.description.abstractThe 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.en_US
dc.subjectSK-RC-52 tumor modelen_US
dc.subjectSmall animal imagingen_US
dc.titleFluorine-18 radiolabeling of a nitrophenyl sulfoxide and its evaluation in an SK-RC-52 model of tumor hypoxiaen_US
dc.typeJournal Articleen_US
dc.identifier.journaltitleJournal of Labelled Compounds and Radiopharmaceuticalsen_US
dc.identifier.affiliationSchool of Chemistry, The University of Melbourne, Melbourne, Victoria, Australiaen_US
dc.identifier.affiliationBio21 Institute, The University of Melbourne, Melbourne, Victoria, Australiaen_US
dc.identifier.affiliationDepartment of Molecular Imaging and Therapy, Austin Health, Heidelberg, Victoria, Australiaen_US
dc.identifier.affiliationOlivia Newton-John Cancer Research Institute, Heidelberg, Victoria, Australiaen_US
dc.identifier.affiliationFaculty of Medicine, Dentistry and Health Sciences, The University of Melbourne, Melbourne, Victoria, Australiaen_US
dc.identifier.affiliationSchool of Cancer Medicine, La Trobe University, Bundoora, Victoria, Australiaen_US
dc.type.austinJournal Articleen_US, Uwe
item.fulltextNo Fulltext-
item.openairetypeJournal Article-
item.grantfulltextnone- Imaging and Therapy- Imaging and Therapy- Newton-John Cancer Research Institute- Imaging and Therapy-
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