Synthesis and Evaluation of F-18 Labeled Pyrido[3,2-B]pyrazine Derivative as a Potential Imaging Agent for Non-Small-Cell Lung Cancer

Pyridopyrazine derivatives have been known as Wnt‐2/β‐catenin signaling pathway inhibitors. Wnt‐2 overexpression may be involved in non‐small‐cell lung cancer (NSCLC). A novel 2‐(4‐[ 18F]fluorobutoxy)‐3‐(phenylethynyl)pyrido[3,2‐b]pyrazine was prepared to demonstrate the feasibility of NSCLC imaging agent by uptake of Wnt‐2 protein. It was synthesized with tosylated precursor using [ 18F]fluoride in radiochemical yield of 44–48%. In cellular uptake evaluation, H460 and H1299, Wnt‐2 expressed cancer cell lines, showed 2.5‐folds higher cellular uptake than that of MCF10A as a control.