Merestinib

Merestinib is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM. It shows more anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than cell lines without MET gene amplification (U-87MG, KATO-III). It shows anti-tumor growth activity in U-87MG, and H441 xenograft models with a dosing of 4 or 12 mg/kg, once or twice daily. It also shows potent inhibitory activity against several other oncogenic proteins, including MST1R, FLT3, AXL, PDGFRA, ROS1, TEK, DDR1/2 and MKNK-1/2.