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179343-17-0

中文名稱 PD089828
英文名稱 PD089828
CAS 179343-17-0
分子式 C18H18Cl2N6O
分子量 405.28
MOL 文件 179343-17-0.mol
更新日期 2024/07/23 09:31:06
179343-17-0 結(jié)構(gòu)式 179343-17-0 結(jié)構(gòu)式

基本信息

中文別名
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
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
英文別名
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)-

物理化學(xué)性質(zhì)

密度1.416±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 25 mg/ml; Ethanol: 1 mg/ml
酸度系數(shù)(pKa)9.85±0.43(Predicted)
形態(tài)固體
顏色White to light yellow

常見(jiàn)問(wèn)題列表

生物活性
PD-089828 是 ATP 競(jìng)爭(zhēng)性 FGFR-1、PDGFR-β 和 EGFR (IC50 分別為 0.15, 1.76, 5.47 μM) 抑制劑和 c-Src 酪氨酸激酶非競(jìng)爭(zhēng)性抑制劑 (IC50=0.18 μM)。PD-089828 也抑制 MAPK,IC50 值為 7.1 μM。PD-089828 體外抑制 PDGF-、EGF- 和 bFGF 介導(dǎo)的酪氨酸激酶受體的自磷酸化。PD-089828 具有持久的細(xì)胞活性。
靶點(diǎn)

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)

體外研究

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.
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