@article{oai:repo.qst.go.jp:00047035, author = {Shimoda, Yoko and Yui, Joji and Fujinaga, Masayuki and Xie, Lin and Kumata, Katsushi and Yamasaki, Tomoteru and Hatori, Akiko and Ogawa, Masanao and Kawamura, Kazunori and Zhang, Ming-Rong and 下田 陽子 and 由井 譲二 and 藤永 雅之 and 謝 琳 and 熊田 勝志 and 山崎 友照 and 羽鳥 晶子 and 小川 政直 and 河村 和紀 and 張 明栄}, issue = {15}, journal = {Bioorganic & Medicinal Chemistry Letters}, month = {Jun}, note = {CEP-32496 is a novel, orally active serine/threonine-protein kinase B-raf (BRAF) (V600E) kinase inhibitor that is being investigated in clinical trials for the treatment of some cancers in patients. In this study, we developed [11C-carbonyl]CEP-32496 as a novel positron emission tomography (PET) probe to study its biodistribution in the whole bodies of mice. [11C]CEP-32496 was synthesized by the reaction of 5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-amine hydrochloride (1·HCl) with [11C]phosgene, followed by treatment with 3-(6,7-dimethoxyquinozolin-4-yloxy)aniline (2). Small-animal PET studies with [11C]CEP-32496 indicated that radioactivity levels (AUC0–90 min, SUV × min) accumulated in the brains of P-gp/BCRP knockout mice at a 8-fold higher rate than in the brains of wild-type mice.}, pages = {3574--3577}, title = {[11C]CEP-32496: radiosynthesis, biodistribution and PET study of brain uptake in P-gp/Bcrp knockout mice}, volume = {24}, year = {2014} }