PD089828

生物活性靶点体外研究 PD089828 试剂级价格

PD089828

CAS号:179343-17-0
英文名:PD089828
中文名:PD089828
CBNumber:CB62731117
分子式:C18H18Cl2N6O
分子量:405.28
MOL File:179343-17-0.mol

PD089828化学性质

密度 :1.416±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 25 mg/ml; Ethanol: 1 mg/ml
形态 :A solid
酸度系数(pKa) :9.85±0.43(Predicted)
颜色 :White to light yellow

PD089828性质、用途与生产工艺

生物活性 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。

靶点

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)

体外研究

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.