1-(2,4-ジフルオロフェニル)-3-{4-[(6,7-ジメトキシキノリン-4-イル)オキシ]-2-フルオロフェニル}尿素 化学特性,用途語,生産方法
外観
白色～うすい褐色, 結晶～粉末
溶解性
ジメチルスルホキシドに可溶
使用
Ki8751 is a potent and selective inhibitor of VEGFR2, PDGFRα and c-Kit with IC50 of 0.9 nM, 67 nM and 40 nM, respectively.
一般的な説明
A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC
50 = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC
50 = 4.0 nM in kinase reactions) assays. It inhibits c-Kit, PDGFRα, and FGFR-2 only at much higher concentrations (IC
50 = 40, 67, and 170 nM, respectively, in cell-based assays), while exhibiting no effect against eight other commonly studied receptor and non-receptor kinases even at concentrations as high as 10 μM. Effectively blocks VEGF-dependent, but not VEGF-independent, cell proliferation
in vitro and tumor growth in mice and rats (5 to 20 mg/kg, daily p.o.)
in vivo.
生物活性
Potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC 50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFR α and FGFR-2 (IC 50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC 50 > 10000 nM for FGFR-2, EGFR and HGFR). Inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo ; antiangiogenic.
1-(2,4-ジフルオロフェニル)-3-{4-[(6,7-ジメトキシキノリン-4-イル)オキシ]-2-フルオロフェニル}尿素 上流と下流の製品情報
原材料
準備製品