[11C]GSK2126458 和 [18F]GSK2126458，用于癌症中 PI3K 和 mTOR 成像的新型潜在 PET 药物的首次放射性标记合成。
[11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers.
机构信息
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1569-74. doi: 10.1016/j.bmcl.2011.12.136. Epub 2012 Jan 10.
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.
GSK2126458 是一种高效的磷酸肌醇 3-激酶（PI3K）和雷帕霉素靶蛋白（mTOR）抑制剂，具有皮摩尔至亚纳摩尔的低活性。[(11)C]GSK2126458 和 [(18)F]GSK2126458 是新型潜在的正电子发射断层扫描（PET）剂，用于在癌症中成像 PI3K 和 mTOR，首次设计并以 40-50%和 20-30%的放射性化学产率、370-740 和 37-222GBq/μmol 的比活度在结束时合成（EOB）。
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