Gefitinib is an approved anticancer drug inhibiting epidermal growth factor receptor/tyrosine kinase(EGFR/TK) in non-small cell lung cancer(NSCLC).In this work

we aimed at developing an auto-synthesis method for 11C-Gefitinib with 11C-CH3-Triflate as methylation agent

and evaluating 11C-Gefinitib to explore its specific uptake with micro PET imaging.11C-Gefitinib was synthesized by the reaction of 7-demethyl precursor with 11C-CH3-Triflate under base condition

and purified by HPLC.Micro PET/CT imaging was performed in A549 tumor-bearing mice.The results showed that it took 28 min for synthesis of 11C-Gefitinib with radiochemical yields of 30%-35%(with decay correction

n>5).The radiochemical purity was over 99%

and the specific activity was 55.5 GBq/μmol

respectively.Micro PET/CT imaging showed that the A549 tumor uptake of 11C-Gefitinib could be blocked by co-injection of non-radioactive Gefitinib(50 mg/kg)

demonstrating the tumor specific accumulation of 11C-Gefitinib.It is concluded that 11C-Gefitinib can be served as PET imaging agent for the evaluation of Gefinitib therapy in NSCLC.