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Wiley, ChemBioChem, 19(24), 2023

DOI: 10.1002/cbic.202300354

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Perfluoro‐tert‐butyl Group‐Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in <sup>19</sup>F Magnetic Resonance Imaging

Journal article published in 2023 by Xinnan Zhang, Luting Wang ORCID, Ruimin Huang ORCID, Jingbo Wang ORCID, Qifan Yan ORCID
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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Abstract

AbstractCapmatinib is an FDA‐approved drug to treat metastatic non‐small cell lung cancer with MET‐exon 14 skipping. Herein, the perfluoro‐tert‐butyl group, which possesses nine chemically identical fluorine atoms, was introduced on Capmatinib to afford a targeted 19F magnetic resonance imaging (MRI) probe, perfluoro‐tert‐butyl group‐derived Capmatinib (9F‐CAP). The 19F MRI concentration limit was found to be 25 mM in FLASH sequence. Molecular docking simulation, surface plasmon resonance (SPR) (with a Kd of 40.7 μM), half‐inhibitory concentration (with a IC50 of 168 nM), Annexin V, and cytotoxicity assays jointly demonstrated that the 9F‐CAP targeted cMET protein specifically. Therefore, the targeted imaging capability of 9F‐CAP is of great significance for the preoperative diagnosis of specific cancers.