Literature DB >> 32631560

Synthesis and evaluation of 18F labeled crizotinib derivative [18F]FPC as a novel PET probe for imaging c-MET-positive NSCLC tumor.

Qingyu Lin1, Yingying Zhang2, Zhequan Fu2, Bingxin Hu2, Zhan Si2, Yanzhao Zhao2, Hongcheng Shi3, Dengfeng Cheng4.   

Abstract

c-MET-positive NSCLC is an important subtype accounting for about 5%~22% of lung cancer. NSCLC patients with activating c-MET are intensively sensitive to c-MET selective receptor tyrosine kinase (RTK) inhibitors, so we aimed to develop a specific PET probe targeting to c-MET-positive NSCLC for potential patients screened by PET/CT. Herein, PET tracer 18F-radiolabeled crizotinib derivative ([18F]FPC) was successfully achieved through a simple one-step 18F-labeling method. [18F]FPC PET imaging on c-MET-positive (as well as blocking group) and negative NSCLC models were further evaluated, and results showed that [18F]FPC was effective as a PET imaging probe that targeted c-MET-positive tumor. Therefore, [18F]FPC could be a potential PET imaging probe for NSCLC tumor which was sensitive to c-MET-TKIs. By virtue of this property, it will benefit NSCLC patients for c-MET-TKI treatment.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cellular-mesenchymal to epithelial transition factor (c-MET); Crizotinib; Non-small-cell lung carcinoma (NSCLC); Positron emission tomography (PET); [(18)F]FPC

Mesh:

Substances:

Year:  2020        PMID: 32631560     DOI: 10.1016/j.bmc.2020.115577

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

1.  Development of a Promising 18F-Radiotracer for PET Imaging Legumain Activity In Vivo.

Authors:  Chunmei Lu; Xiuting Wang; Qiqi Wang; Lixia Zhang; Jianguo Lin; Ling Qiu
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-27

Review 2.  Recent progress in the imaging of c-Met aberrant cancers with positron emission tomography.

Authors:  Giuseppe Floresta; Vincenzo Abbate
Journal:  Med Res Rev       Date:  2022-03-16       Impact factor: 12.388

  2 in total

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