521238
PDGFRβ/RAF Kinase Inhibitor
The PDGFRβ/RAF Kinase Inhibitor controls the biological activity of PDGFRβ/RAF Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
PDGFRβ/RAF Kinase Inhibitor, PDGFR Tyrosine Kinase Inhibitor XXII, 6-(4-(5-(3-(Trifluoromethyl)phenylamino)-4 H-1,2,4-triazol-3-yl)phenoxy)-2-(methylthio)pyrimidin-4-amine
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About This Item
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质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
beige
溶解性
DMSO: soluble
运输
ambient
储存温度
−20°C
SMILES字符串
NC1=CC(OC2=CC=C(C3=NN=C(NC4=CC(C(F)(F)F)=CC=C4)N3)C=C2)=NC(SC)=N1
一般描述
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).
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Murphy, E.A., et al. 2010. Proc. Natl. Acad. Sci. USA107, 4299.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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