产品描述
| 溶解性 | Soluble in DMSO (21 mg/ml), ethanol (100 mM), water (partly miscible), methanol, and chloroform. |
| 存贮条件 | 储存温度-20°C |
| 应用 | Potent inhibitor of FGF and VEGF (Flt/Flk) receptors. |
| 产品介绍 | PD173074是一种有效的FGFR1抑制剂，IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。 |
| 备注 | PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src. |
| 生化机理 | FGF/VEGF Receptor Tyrosine Kinase Inhibitor, PD173074 is a cell-permeable pyridopyrimidine compound that has been shown to act as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors {IC50 = 21.5 nM for Flg (FGFR1)}. It has been used to inhibit PDGFR and c-Src only at much higher concentration (IC50 = 17.6 μM, 19.8 μM, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 μM. It has also been shown to inhibit the autophosphorylation of endogenous Flg (FGFR1, IC50 <5 nM) and overexpressed Flk-1 (VEGFR2, IC50 <200 nM) in NIH3T3 cells in vitro. Inhibition of FGFR signaling impairs angiogenesis as well as self-renewal of stem cells via ERK1/2 activation. Also indicated as an inhibitor of FGFR-3. |
| 别名 | N-[2-[[4-(二乙基氨基)丁基]氨基]-6-(3,5-二甲氧基苯基)吡啶并[2,3-d]嘧啶-7-基]-N'-叔丁基脲;PD 173074;PD-173074;N-[2-[[4-(Diethylamino)butyl]amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N′-(1,1-dimethylethyl)urea |
