|
PDGFRβ/RAF Kinase Inhibitor
6-(4-(5-(3-(Trifluoromethyl)phenylamino)-4 H-1,2,4-triazol-3-yl)phenoxy)-2-(methylthio)pyrimidin-4-amine , PDGFR Tyrosine Kinase Inhibitor XXII
An orally bioavailable amino-triazole compound that is shown to bind to the inactive conformations of both PDGFRβ and Raf kinases (allosteric, Type II inh), and acts as a potent inhibitor of Flt3, Kit, PDGFRα and PDGFRβ (Kd = 52, 170, 300 and 520 nM, respectively) with selectivity over B-Raf, p38α, FGFR2 and VEGFR2 (Kd > 10 µM) in a multi-kinase panel. Completely blocks the phosphorylations of MEK-1/2 S217/S221, ERK-1/2 T202/Y204 in FGF-stimulated HUVECs, PDGFRβ in PDGF-BB-stimulated VSMCs, ERK-1/2 T202/Y204 in 1205Lu-B Raf V600E cells, and C-Raf S338 at 10 µM. Reduces FGF-induced angiogenesis in mouse Matrigel model (50 mg/kg, i.p., bid) and selectively induces apoptosis in the endothelium; further, suppresses orthotopic renal cell carcinoma growth in mice (100 mg/kg, p.o., qd).
产品信息
Form Beige solid
Molar mass 459.6
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C20H16F3N7OS
商店和运输信息
Storage -20°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |