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PD-161570
CAS No. : 192705-80-9
MCE 国际站：PD-161570
产品活性：PD-161570 是一种有效的且具有 ATP 竞争能力的人 FGF-1 受体抑制剂，IC50 为 39.9 nM，Ki 为 42 nM。PD-161570 还抑制 PDGFR，EGFR 和 c-Src 酪氨酸激酶，IC50 值分别为 310 nM，240 nM 和 44 nM。PD-161570 抑制 PDGF 刺激的自磷酸化和 FGF-1 受体磷酸化，IC50 分别为 450 nM 和 622 nM。PD-161570 还是一种骨形态发生蛋白 (BMPs) 和 TGF-β 信号抑制剂。
研究领域：Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | TGF-beta/Smad
作用靶点：FGFR | PDGFR | EGFR | Src | TGF-β Receptor
In Vitro: PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC50 of 0.3 µM on day 8.
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture.
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis.
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文献和实验一般 抑郁症 CUMS，脑嗅球损伤法 大小鼠 90% 简单 非常耗时 脓毒症模型 盲肠穿刺 大小鼠 80%-90% 简单 一般 阿尔兹海默模型 D-半乳糖诱导 KM小鼠 70%-80% 简单 较耗时 帕金森模型 (PD) 利血平，6-OHDA，MPTP Wistar大鼠 70%-80% 简单 较耗时
.5 0.714 1-己炔 CH3(CH2)3C≡CH -132 71 0.715 2-己炔 CH3(CH2)2C≡CH -88 84 0.730 3-己炔 CH3CH2C≡CCH3 -51 81.8 0.724 1-庚炔 CH3(CH2)4C≡CH -81 100 0.734 2-庚炔 CH3(CH2)3C≡CCH3 - 112 0.748 3-庚炔 CH3(CH2)2C≡CCH3 - 105 0.752 1-辛炔 CH3(CH2)5C≡CH -80 125.2 0.746 2-辛炔 CH3(CH2)4C≡
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