[11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers.
GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity. [(11)C]GSK2126458 and [(18)F]GSK2126458, 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 37-222GBq/μmol specific activity at end of bombardment (EOB), respectively.
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Min
M
Wang
Mingzhang
M
Gao
Kathy D
KD
Miller
George W
GW
Sledge
Qi-Huang
QH
Zheng
D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D019788:Fluorodeoxyglucose F18 / Q000493:pharmacokinetics; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis* / Q000000981:diagnostic imaging; D019869:Phosphatidylinositol 3-Kinases / Q000032:analysis* / Q000378:metabolism; D049268:Positron-Emission Tomography; D011724:Pyridazines; D011804:Quinolines / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D013449:Sulfonamides / Q000737:chemistry*; D058570:TOR Serine-Threonine Kinases / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism; D000096926:Benzenesulfonamides
D002250:Carbon Radioisotopes; D019788:Fluorodeoxyglucose F18; D019869:Phosphatidylinositol 3-Kinases; D011724:Pyridazines; D011804:Quinolines; D019275:Radiopharmaceuticals; D013449:Sulfonamides; D058570:TOR Serine-Threonine Kinases; C561454:omipalisib; D000096926:Benzenesulfonamides; C546842:MTOR protein, human