PD089828

PD089828

中文名称PD089828
中文同义词N-[2-氨基-6-(2,6-二氯苯基)吡啶基[2,3-d]嘧啶-7-基]-N'-叔丁基脲;1-(2-氨基-6-(2,6-二氯苯基)吡啶并[2,3-D]嘧啶-7-基)-3-叔丁基脲;化合物PD 089828
英文名称PD089828
英文同义词PD089828;1-(2-Amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-(tert-butyl)urea;Urea, N-[2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)-;EGFR,ATP,nonselective,PD 089828,PDGFR,autophosphorylation,PD089828,HER1,Epidermal growth factor receptor,ErbB-1,phosphorylation,vascular,antiproliferative,smooth,antimigratory,competitive,Inhibitor,Platelet-derived growth factor receptor,PD-089828,Src,muscle,cells,FGFR,inhibit,Fibroblast growth factor receptor
CAS号179343-17-0
分子式C18H18Cl2N6O
分子量405.28
EINECS号
相关类别化工
Mol文件179343-17-0.mol
结构式PD089828 结构式

PD089828 性质

密度1.416±0.06 g/cm3(Predicted)
储存条件Store at -20°C
溶解度DMSO:25mg/mL;乙醇:1mg/mL
形态固体
酸度系数(pKa)9.85±0.43(Predicted)

PD089828 用途与合成方法

PD-089828 是 ATP 竞争性 FGFR-1、PDGFR-β 和 EGFR (IC50 分别为 0.15, 1.76, 5.47 µM) 抑制剂和 c-Src 酪氨酸激酶非竞争性抑制剂 (IC50=0.18 µM)。PD-089828 也抑制 MAPK,IC50 值为 7.1 µM。PD-089828 体外抑制 PDGF-、EGF- 和 bFGF 介导的酪氨酸激酶受体的自磷酸化。PD-089828 具有持久的细胞活性。

FGFR1

0.15 μM (IC 50 )

PDGFR-β

1.76 μM (IC 50 )

EGFR

5.47 μM (IC 50 )

c-Src

0.18 μM (IC 50 )

FGFR1

0.14 μM (Ki)

PDGFR-β

2.38 μM (Ki)

EGFR

3.16 μM (Ki)

c-Src

0.1 μM (Ki)

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC 50 of 0.82 µM.
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC 50 value of 10.9 µM.
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC 50 value of 0.63 µM. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC 50 value of 1.8 µM.
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC 50 values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis.

Cell Proliferation Assay

Cell Line: Vascular smooth muscle cells (serum-stimulated growth)
Concentration: 10 µM
Incubation Time: 8 consecutive days
Result: Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.

Western Blot Analysis

Cell Line: Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
Concentration: 0.5-20 µM
Incubation Time: 2 hours
Result: Inhibited PDGFR autophosphorylation with an IC 50 of 0.82 µM.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-112345PD-0898281 mg360元
2024/04/30HY-112345PD089828
PD-089828
179343-17-05 mg900元
"PD089828"相关产品信息
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