PD-161570;PF-1480232
中文名称 | PD-161570;PF-1480232 |
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中文同义词 | 1-(叔丁基)-3-(6-(2,6-二氯苯基)-2-((4-(二乙基氨基)丁基)氨基)吡啶并[2,3-D]嘧啶-7-基)脲;化合物PD 161570;PD-161570,FGFR抑制剂 |
英文名称 | N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea |
英文同义词 | N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea;PD 161570;1-Tert-butyl-3-[6-(2,6-dichloro-phenyl)-2-(4-diethylaMino-butylaMino)pyrido[2,3-d]pyriMidin-7-yl]urea;PF-1480232;PD-161570;PF-1480232;1-(tert-Butyl)-3-(6-(2,6-dichlorophenyl)-2-((4-(diethylamino)butyl)amino)pyrido[2,3-d]pyrimidi;Inhibitor,Fibroblast growth factor receptor,HER1,kinases,autophosphorylation,PDGFR,PD161570,FGFR,Src,inhibit,TGF-β Receptor,ATP-competitive,Epidermal growth factor receptor,tyrosine,Platelet-derived growth factor receptor,disease,EGFR,anti-cancer,angiogenesis,ErbB-1,FGFR1,Transforming growth factor beta receptors,cardiovascular,anti-proliferation,PD-161570;Urea, N-[6-(2,6-dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)- |
CAS号 | 192705-80-9 |
分子式 | C26H35Cl2N7O |
分子量 | 532.51 |
EINECS号 | |
相关类别 | 合成;Aromatics;Bases & Related Reagents;Heterocycles;Intermediates & Fine Chemicals;Nucleotides;Pfizer compounds;Pharmaceuticals;Tyrosine Kinase Inhibitors |
Mol文件 | 192705-80-9.mol |
结构式 |
PD-161570;PF-1480232 性质
熔点 | 215-230?C |
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密度 | 1.249±0.06 g/cm3(Predicted) |
储存条件 | Store at RT |
溶解度 | 二甲基亚砜:>10mg/mL |
形态 | 粉末 |
酸度系数(pKa) | 9.82±0.43(Predicted) |
颜色 | 白色至类白色 |
FGFR1 39.9 nM (IC 50 ) |
FGFR1 42 nM (Ki) |
FGFR1 autophosphorylation 622 nM (IC 50 ) |
PDGFRβ 262 nM (IC 50 ) |
PDGFR 310 nM (IC 50 ) |
EGFR 240 nM (IC 50 ) |
c-Src 44 nM (IC 50 ) |
TGF-β Receptor
|
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 IC
50
of 0.3 µM on day 8.
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A
121(p)
) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A
121(p)
cells in culture.
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis.
Cell Proliferation Assay
Cell Line: | Vascular smooth muscles cells (VSMCs) |
Concentration: | 0.1 µM, 0.3 µM, 1 µM |
Incubation Time: | 1 day, 3 days, 6 days, 8 days |
Result: | Inhibited VSMC proliferation in a dose dependent fashion with an IC 50 of 0.3 µM at day 8. |
安全信息
危险品标志 | T |
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危险类别码 | 25-36/37/38 |
安全说明 | 26-45 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-100434 | PD-161570 | 1 mg | 1028元 | |
2024/04/30 | P2531 | PD-161570;PF-1480232 PD-161570 | 192705-80-9 | 25MG | 1555元 |