[11C-carbonyl]CEP-32496: Radiosynthesis, biodistribution and PET study of brain uptake in P-gp/BCRP knockout mice
作者： Yoko Shimoda , Joji Yui , Masayuki Fujinaga , Lin Xie , Katsushi Kumata
DOI: 10.1016/J.BMCL.2014.05.045
关键词:
摘要: CEP-32496 is a novel, orally active serine/threonine-protein kinase B-raf (BRAF) (V600E) inhibitor that being investigated in clinical trials for the treatment of some cancers patients. In this study, we developed [(11)C-carbonyl]CEP-32496 as novel positron emission tomography (PET) probe to study its biodistribution whole bodies mice. [(11)C]CEP-32496 was synthesized by reaction 5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-amine hydrochloride (1·HCl) with [(11)C]phosgene, followed 3-(6,7-dimethoxyquinozolin-4-yloxy)aniline (2). Small-animal PET studies indicated radioactivity levels (AUC0-90 min, SUV×min) accumulated brains P-gp/BCRP knockout mice at 8-fold higher rate than wild-type
sci-hub.se 参考文章(24)
Ju-Han Lee, Eung-Seok Lee, Young-Sik Kim, Clinicopathologic significance of BRAF V600E mutation in papillary carcinomas of the thyroid: a meta-analysis. Cancer. ,vol. 110, pp. 38- 46 ,(2007) , 10.1002/CNCR.22754
T Conway, M Diksic, Synthesis of “No-Carrier-Added” Carbon-11 SarCNU: The Sarcosinamide Analog of the Chemotherapeutic Agent BCNU The Journal of Nuclear Medicine. ,vol. 29, pp. 1957- 1960 ,(1988)
Yuuki Takada, Masanao Ogawa, Hisashi Suzuki, Toshimitsu Fukumura, Radiosynthesis of [2-11C-carbonyl]dantrolene using [11C]phosgene for PET Applied Radiation and Isotopes. ,vol. 68, pp. 1715- 1720 ,(2010) , 10.1016/J.APRADISO.2010.03.012
S. Harmsen, I. Meijerman, R.F. Maas-Bakker, J.H. Beijnen, J.H.M. Schellens, PXR-mediated P-glycoprotein induction by small molecule tyrosine kinase inhibitors. European Journal of Pharmaceutical Sciences. ,vol. 48, pp. 644- 649 ,(2013) , 10.1016/J.EJPS.2012.12.019
Philip Murphy, Mats Bergstrom, Radiopharmaceuticals for oncology drug development: a pharmaceutical industry perspective. Current Pharmaceutical Design. ,vol. 15, pp. 957- 965 ,(2009) , 10.2174/138161209787581977
Chiharu Asakawa, Masanao Ogawa, Katsushi Kumata, Masayuki Fujinaga, Koichi Kato, Tomoteru Yamasaki, Joji Yui, Kazunori Kawamura, Akiko Hatori, Toshimitsu Fukumura, Ming-Rong Zhang, [11C]sorafenib: radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice. Bioorganic & Medicinal Chemistry Letters. ,vol. 21, pp. 2220- 2223 ,(2011) , 10.1016/J.BMCL.2011.03.002
Kazunori Kawamura, Tomoteru Yamasaki, Fujiko Konno, Joji Yui, Akiko Hatori, Kazuhiko Yanamoto, Hidekatsu Wakizaka, Makoto Takei, Yuichi Kimura, Toshimitsu Fukumura, Ming-Rong Zhang, Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [(11)C]GF120918 by PET in mice. Molecular Imaging and Biology. ,vol. 13, pp. 152- 160 ,(2011) , 10.1007/S11307-010-0313-1
Masanao Ogawa, Yuuki Takada, Hisashi Suzuki, Kazuyoshi Nemoto, Toshimitsu Fukumura, Simple and effective method for producing [11C]phosgene using an environmental CCl4 gas detection tube. Nuclear Medicine and Biology. ,vol. 37, pp. 73- 76 ,(2010) , 10.1016/J.NUCMEDBIO.2009.08.008
Ming-Rong Zhang, Katsushi Kumata, Akiko Hatori, Nobuhiko Takai, Jun Toyohara, Tomoteru Yamasaki, Kazuhiko Yanamoto, Joji Yui, Kazunori Kawamura, Sachiko Koike, Koichi Ando, Kazutoshi Suzuki, [11C]Gefitinib ([11C]Iressa): Radiosynthesis, In Vitro Uptake, and In Vivo Imaging of Intact Murine Fibrosarcoma Molecular Imaging and Biology. ,vol. 12, pp. 181- 191 ,(2010) , 10.1007/S11307-009-0265-5
Chiharu Asakawa, Masanao Ogawa, Katsushi Kumata, Masayuki Fujinaga, Tomoteru Yamasaki, Lin Xie, Joji Yui, Kazunori kawamura, Toshimitsu Fukumura, Ming-Rong Zhang, Radiosynthesis of three [11C]ureido-substituted benzenesulfonamides as PET probes for carbonic anhydrase IX in tumors. Bioorganic & Medicinal Chemistry Letters. ,vol. 21, pp. 7017- 7020 ,(2011) , 10.1016/J.BMCL.2011.09.102