Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM.
Tivantinib (ARQ-197) has no inhibition for EGFR, InsR, PDGFRα, FGFR1 and FGFR4 etc., only modest inhibition (35%) for Ron at 30 uM.
Tivantinib (ARQ-197) inhibits constitutive c-Met phosphorylation in HT29 and MKN-45 cells, and HGF-induced c-Met phosphorylation in MDA-MB-231 and NCI-H441 cells with IC50 of 100-300 nM.
Tivantinib (ARQ-197) shows antiproliferative activity against multiple cancer cell lines (IC50=0.03-30 uM).
Tivantinib (ARQ-197) exerts tumor growth inhibition in multiple mouse xenograft; orally active.
