Synthesis and in vivo evaluation of [11C]tucatinib for HER2-targeted PET imaging

Marius Müller,Vladimir Shalgunov,Lars Hvass,Jesper T Jørgensen,Vasko Kramer,Markus Staudt,Umberto Maria Battisti,Andreas Kjaer,Matthias M Herth

Bioorganic & Medicinal Chemistry Letters（2023）

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摘要

•[11C]tucatinib was designed and synthesized as a HER2 PET imaging agent•The compound was obtained in a 12 steps synthetic route•[11C]tucatinib was obtained in good radiochemical yield and high radiochemical purity•[11C]tucatinib showed high liver and intestinal uptake and low tumor uptake•Modifications of [11C]tucatinib are required to obtain a successful HER2 PET tracer

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关键词

Breast cancer,HER2,Tucatinib,PET imaging,Radiolabeling,Carbon-11

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