Derazantinib (ARQ-087) is a novel potent, ATP competitive multi-kinase inhibitor with IC50 of FGFR1/2/3 with IC50 of 1.8-4.5 nM.
Derazantinib (ARQ-087) also inhibits FGFR4, Src, Abl, RET, etc. (IC50<50 nM).
Derazantinib (ARQ-087) inhibits FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK), shows potent anti-proliferative effect in cell lines driven by FGFR dysregulation.
Derazantinib (ARQ-087) shows tumor growth inhibition in vivo in xenograft tumor models.
