PD-161570;PF-1480232

PD-161570;PF-1480232

中文名称PD-161570;PF-1480232
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 结构式

PD-161570;PF-1480232 性质

熔点215-230?C
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

PD-161570;PF-1480232 用途与合成方法

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。

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
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 Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-100434PD-1615701 mg1028元
2024/04/30P2531PD-161570;PF-1480232
PD-161570
192705-80-925MG1555元

PD-161570;PF-1480232 上下游产品信息

"PD-161570;PF-1480232"相关产品信息
哌嗪-N,N'-二(2-乙磺酸)
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