Affiliation:
1. Key Laboratory for Advanced Materials and Feringa Nobel Prize Scientist Joint Research Center School of Chemistry and Molecular Engineering East China University of Science and Technology 130 Meilong Rd. Shanghai 200237 China
2. Shanghai Institute of Materia Medica Chinese Academy of Sciences 555 Zuchongzhi Rd. Shanghai 201203 China
3. Shanghai Ninth People's Hospital Shanghai Jiaotong University School of Medicine 639 Zhizaoju Rd. Shanghai 200025 China
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.
Funder
Fundamental Research Funds for the Central Universities
Subject
Organic Chemistry,Molecular Biology,Molecular Medicine,Biochemistry