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PD173074
点击次数:446发布时间:2013/4/1 15:57:11
更新日期:2022/8/19 17:45:40
所 在 地:美洲
产品型号:
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详细内容
PD173074
上海义森生物科技有限公司
技术数据:
分子量(MW): 523.67 化学式: C28H41N7O3
溶解度: DMSO 105mg/mL Water <1mg/mL Ethanol 105mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 219580-11-7
生物活性
PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.PD173074 is a cell-permeable pyridopyrimidine compound. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. PD173074 inhibits 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. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50 <5 nM) and overexpressed VEGFR2 (IC50 <200 nM) in NIH3T3 cells in vitro, and FGF- and VEGF-induced angiogenesis in mice in vivo. [1][2]
技术数据:
分子量(MW): | 523.67 | |
---|---|---|
化学式: | C28H41N7O3 | |
溶解度: | DMSO 105mg/mL Water <1mg/mL Ethanol 105mg/mL | |
纯度: | >99% | |
稳定性: | at -20℃ 2 years | |
CAS号: | 219580-11-7 |
生物活性
PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.PD173074 is a cell-permeable pyridopyrimidine compound. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. PD173074 inhibits 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. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50 <5 nM) and overexpressed VEGFR2 (IC50 <200 nM) in NIH3T3 cells in vitro, and FGF- and VEGF-induced angiogenesis in mice in vivo. [1][2]