Description
BMS 777607 can inhibit c-Met with IC50 of 20 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C25H19ClF2N4O4
Chemical Name
N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Solubility
DMSO 47 mg/mL Water
In vitro
BMS-777607 is a novel, selective, and orally available ATP-competitive Met kinase inhibitor that specifically targets several Met family members and potently binds to the c-Met active site with a Ki value of 3.9 nmol/L. BMS-777607 potently blocked the autophosphoryla-tion of c-Met with an IC 50 of 20 nmol/L. BMS-777607 can inhibit HGF-induced prostate cancer cell scattering, suppress HGF-induced cell migration, impair HGF-mediated cell invasion and reduce cell proliferation increased by HGF. BMS-777607 can also block HGF-stimulated c-Met downstream signaling pathway
In vivo
Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity.
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