Solid. Soluble in DMSO. LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R and other oncoproteins. It displays anti-tumour activities in mouse xenograft models. In vitro, LY2801653 has an IC50 for inhibition of MET phosphorylation between 35.2-59.2nM. LY2801653 was...

LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM). It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s =...

Description: Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell...