Radiosynthesis of 3′-deoxy-3′-[18F]fluorothymidine:: [18F]FLT for imaging of cellular proliferation in vivo

被引：167
|
作者：
Grierson, JR
Shields, AF
机构：
[1] Univ Washington, Med Ctr, Res Imaging Lab, Seattle, WA 98195 USA
[2] Wayne State Univ, Harper Hosp, Karamanos Canc Inst, Detroit, MI USA
来源：
NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 02期
关键词：
F-18]FLT; 3 ' deoxy-3 '-flourothymidine; DNA synthesis; PET imaging; proliferation; fluorine-18; TK-1; thymidine kinase; thymidine metabolism; C-11]thymidine;
D O I：
10.1016/S0969-8051(99)00104-3
中图分类号：
R8 [特种医学]; R445 [影像诊断学];
学科分类号：
1002 ; 100207 ; 1009 ;
摘要：
A reliable radiosynthesis of 3'-deoxy-3'-[F-18]fluorothymidine ([F-18]FLT) has been developed based on [F-18]fluoride displacement of a protected nosylate precursor. A simple three-step synthesis is described that is useful for preparing >10 mCi (370 MBq) of radiochemically pure [F-18]FLT, with a specific activity >1 Ci/mu mol (37 GBq/mu mol) at EOS within 100 min and in 13% radiochemical yield tend of bombardment (EOB); 7% end of synthesis (EOS). [F-18]FLT has been designed as a new positron emission tomography imaging agent for visualizing cellular proliferation in vivo based on the metabolism of thymidine. NUCL MED BIOL 27;2:143-156, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.
引用
收藏
页码：143 / 156
页数：14
相关论文
共 50 条
  • [41] Re(CO)3([18F]FEDA), a novel 18F PET renal tracer: Radiosynthesis and preclinical evaluation
    Lipowska, Malgorzata
    Jarkas, Nashwa
    Voll, Ronald J.
    Nye, Jonathon A.
    Klenc, Jeffrey
    Goodman, Mark M.
    Taylor, Andrew T.
    NUCLEAR MEDICINE AND BIOLOGY, 2018, 58 : 42 - 50
  • [42] Reproducibility of 18F-FDG and 3′-Deoxy-3′-18F-Fluorothymidine PET Tumor Volume Measurements
    Hatt, Mathieu
    Rest, Catherine Cheze-Le
    Aboagye, Eric O.
    Kenny, Laura M.
    Rosso, Lula
    Turkheimer, Federico E.
    Albarghach, Nidal M.
    Metges, Jean-Philippe
    Pradier, Olivier
    Visvikis, Dimitris
    JOURNAL OF NUCLEAR MEDICINE, 2010, 51 (09) : 1368 - 1376
  • [43] Efficient Radiosynthesis of 3′-Deoxy-3′-18F-Fluorothymidine Using Electrowetting-on-Dielectric Digital Microfluidic Chip
    Javed, Muhammad Rashed
    Chen, Supin
    Kim, Hee-Kwon
    Wei, Liu
    Czernin, Johannes
    Kim, Chang-Jin CJ
    Dam, R. Michael van
    Keng, Pei Yuin
    JOURNAL OF NUCLEAR MEDICINE, 2014, 55 (02) : 321 - 328
  • [44] Gemcitabine Mechanism of Action Confounds Early Assessment of Treatment Response by 3′-Deoxy-3′-[18F]Fluorothymidine in Preclinical Models of Lung Cancer
    Schelhaas, Sonja
    Held, Annelena
    Wachsmuth, Lydia
    Hermann, Sven
    Honess, Davina J.
    Heinzmann, Kathrin
    Smith, Donna-Michelle
    Griffiths, John R.
    Faber, Cornelius
    Jacobs, Andreas H.
    CANCER RESEARCH, 2016, 76 (24) : 7096 - 7105
  • [45] Early assessment of tumor response to JAC106, an anti-tubulin agent, by 3′-deoxy-3′-[18F]fluorothymidine in preclinical tumor models
    Lee, Seung Jin
    Kang, Hye Young
    Kim, Seog Young
    Chung, Jin Hwa
    Oh, Seung Jun
    Ryu, Jin-Sook
    Kim, Sung-Bae
    Kang, Jong Soon
    Park, Song-Kyu
    Kim, Hwan Mook
    Kim, Myung-Hwa
    Moon, Dae Hyuk
    EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2011, 38 (08) : 1436 - 1448
  • [46] Radiosynthesis and Preclinical Evaluation of m-[18F]FET and [18F]FET-OMe as Novel [18F]FET Analogs for Brain Tumor Imaging
    Groener, Benedikt
    Hoffmann, Chris
    Endepols, Heike
    Urusova, Elizaveta A.
    Brugger, Melanie
    Neumaier, Felix
    Timmer, Marco
    Neumaier, Bernd
    Zlatopolskiy, Boris D.
    MOLECULAR PHARMACEUTICS, 2024, 21 (06) : 2795 - 2812
  • [47] Clinical value of 3'-deoxy-3'-[18F]fluorothymidine-positron emission tomography for diagnosis, staging and assessing therapy response in lung cancer
    Alwadani, Bandar
    Dall'Angelo, Sergio
    Fleming, Ian N.
    INSIGHTS INTO IMAGING, 2021, 12 (01)
  • [48] USE OF 3'-DEOXY-3'-[18F]FLUOROTHYMIDINE PET/CT FOR EVALUATING RESPONSE TO CYTOTOXIC CHEMOTHERAPY IN DOGS WITH NON-HODGKIN'S LYMPHOMA
    Lawrence, Jessica
    Vanderhoek, Matthew
    Barbee, David
    Jeraj, Robert
    Tumas, Daniel B.
    Vail, David M.
    VETERINARY RADIOLOGY & ULTRASOUND, 2009, 50 (06) : 660 - 668
  • [49] Altered Tissue 3′-Deoxy-3′-[18F]Fluorothymidine Pharmacokinetics in Human Breast Cancer following Capecitabine Treatment Detected by Positron Emission Tomography
    Kenny, Laura M.
    Contractor, Kaiyumars B.
    Stebbing, Justin
    Ai-Nahhas, Adil
    Palmieri, Carlo
    Shousha, Sami
    Coombes, R. Charles
    Aboagye, Eric O.
    CLINICAL CANCER RESEARCH, 2009, 15 (21) : 6649 - 6657
  • [50] N3-Substituted thymidine analogues III:: radiosynthesis of N3-[(4-[18F]fluoromethyl-phenyl)butyl]thymidine ([18F]-FMPBT) and N3-[(4-[18F]fluoromethyl-phenyl)pentyl] thymidine ([18F]-FMPPT) for PET
    Ghosh, Pradip
    Gelovani, Juri G.
    Alauddin, Mian M.
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2007, 50 (13-14) : 1185 - 1191
12345