[11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers

Min Wang, Mingzhang Gao, Kathy D. Miller, George W. Sledge, Qi Huang Zheng

Research output: Contribution to journalArticle

48 Scopus citations

Abstract

GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity. [11C]GSK2126458 and [18F]GSK212 6458, new potential PET agents for imaging of PI3K and mTOR in cancer, were first designed and synthesized in 40-50% and 20-30% decay corrected radiochemical yield, and 370-740 and 37-222 GBq/lmol specific activity at end of bombardment (EOB), respectively.

Original languageEnglish (US)
Pages (from-to)1569-1574
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number4
DOIs
StatePublished - Feb 15 2012

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Keywords

  • [ C]GSK2126458
  • [ F]GSK2126458
  • Cancer
  • Mammalian target of rapamycin (mTOR)
  • Phosphoinositide 3-kinase (PI3K)
  • Positron emission tomography (PET)

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry
  • Medicine(all)

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