MET inhibitor Compound 1

A novel potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively; demonstrates potent, broad spectrum activity against MET mutants (V1110I, H1112Y, L1195V, Y1235D, D1228H and M1250T) with IC50 of <1 nM-57 nM, and Y1230 mutants with moderate potency (IC50=25-280 nM); displays >50-fold selectivity in a panel of 130 kinases with exception of Fms and TrkA/B/C; inhibits MET-dependent tumor cell growth in vivo through decreasing phosphorylaed MET.

References 1. Farrell PJ, et al. Mol Cancer Ther. 2017 Jul;16(7):1269-1278. View Related Products by Target c-Met (HGFR)