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

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Wang M,Gao M,Miller KD,Sledge GW,Zheng QH

doi

10.1016/j.bmcl.2011.12.136

subject

Has Abstract

pub_date

2012-02-15 00:00:00

pages

1569-74

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00025-X

journal_volume

22

pub_type

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