BJG-03-025

BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.BJG-03-025 demonstrates excellent kinome selectivity was profiled by KINOMEscan screening, PLK1 proved to be a false positive with IC50 of 8.3 uM, 100-300-fold selective for FAK.BJG-03-025 displays antiproliferative activity in three-dimensional (3D)-breast and gastric cancer models and impacts cellular signaling and migration.BJG-03-025 decreased phosphorylated FAK (pFAK Y397) in gastric cancer CDH1–/–RHOAY42C/+ organoid model, decreased aberrant signaling and proliferation of gastric cancer organoids.

1. Brian J Groendyke, et al. ACS Med Chem Lett. 2020 Dec 14;12(1):30-38.