SAR125844

SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC₅₀ is 4.2 nM and K_i is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer^[1][2][3]. IC50 & Target:IC50: 4.2 nM (MET RTK)^[1]. In Vitro:SAR125844 (1-10000 nM, 96 h) inhibits proliferation in H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells^[1].
SAR125844 (1-300 nM, 24 72 h) promotes apoptosis in SNU-5 cells^[1].
SAR125844 (3-1000 nM, 20 h) inhibits HGF-mediated tumor cell migration in PC-3 cells^[1]. In Vivo:SAR125844 (45 mg/kg, Intravenous injection, single dose) results in tumor regression in SNU-5 and Hs 746T tumor-bearing mice^[1].
SAR125844 (20 mg/kg, Intravenous injection, o single dose) nanoformulation results in long duration pharmacodynamic impact and tumor regression in MET-amplified gastric tumor models^[1].
SAR125844 (20 mg/kg, Intravenous injection, single dose) shows MET kinase inhibition was complete at 4 h (96%), significant at 24 h (80%), and partial at 48 h (61%) in mice bearing xenograft tumor of the MET-amplified Hs 746T human gastric tumor cell line^[3].