[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. [11C]GSK2126458 and [18F]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 37–222 GBq/μmol specific activity at end of bombardment (EOB), respectively.

Graphical abstractRadiosynthesis of [11C]GSK2126458 and [18F]GSK2126458, new potential PET agents for imaging of PI3K and mTOR in cancer, is first reported.Figure optionsDownload full-size imageDownload as PowerPoint slide