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

Synthesis and evaluation of 18F labeled crizotinib derivative [18F]FPC as a novel PET probe for imaging c-MET-positive NSCLC tumor. Bioorg Med Chem. 2020 Aug 01;28(15):115577 Authors: Lin Q, Zhang Y, Fu Z, Hu B, Si Z, Zhao Y, Shi H, Cheng D 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. PMID: 32631560 [PubMed - in process]
Source: Bioorganic and Medicinal Chemistry - Category: Chemistry Authors: Tags: Bioorg Med Chem Source Type: research