[ 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 Miller, George W. Sledge, Qi-Huang Zheng

Research output: Contribution to journalArticle

45 Citations (Scopus)

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
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)

Cite this

[ 11C]GSK2126458 and [ 18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers. / Wang, Min; Gao, Mingzhang; Miller, Kathy; Sledge, George W.; Zheng, Qi-Huang.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 22, No. 4, 15.02.2012, p. 1569-1574.

Research output: Contribution to journalArticle

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