Catalog No.: PC-20333Not For Human Use, Lab Use Only.
Merestinib (LY2801653) is a potent, selective, type-II ATP competitive inhibitor of c-Met with Ki of 2 nM, inhibits c-MET wt and mutant Y1230C with IC50 of 42 and 54 nM, respectively.
Merestinib (LY2801653) is a potent, selective, type-II ATP competitive inhibitor of c-Met with Ki of 2 nM, inhibits c-MET wt and mutant Y1230C with IC50 of 42 and 54 nM, respectively.
LY2801653 inhibited MET auto-phosphorylation in HGF-stimulated H460 cells and S114 cells with IC50 of 35.2 and 59.2 nM, resepctively.
LY2801653 inhibited growth of a panel of MET mutated variant clones with an IC50 ranging from 3-fold more potent (V1092I) to approximately 6-fold less potent (L1195V) compared with the growth inhibition of cells with the MET wild-type sequence.
LY2801653 demonstrated more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87MG, KATO-III).
LY2801653 (12 mg/kg, BID, oral) demonstrated in vivo anti-tumor activity in MET-dependent U-87MG and H441 xenograft models.
