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PD-089828

CAS No. : 179343-17-0

MCE 国际站：PD-089828

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling

作用靶点：FGFR  |  PDGFR  |  EGFR  |  Src

In Vitro: PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC₅₀ of 0.82 µM.
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC₅₀ value of 10.9 µM.
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC₅₀ value of 0.63 µM.PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC₅₀ value of 1.8 µM.
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC₅₀ values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis.

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