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

摘要

Pyridopyrazine derivatives have been known as Wnt-2/beta-catenin signaling pathway inhibitors. Wnt-2 overexpression may be involved in non-small-cell lung cancer (NSCLC). A novel 2-(4-[F-18]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 [F-18]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.