1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. FGFR
    PDGFR
    EGFR
    Src
  3. PD-089828

PD-089828 

Cat. No.: HY-112345
Handling Instructions

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD 089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro.

For research use only. We do not sell to patients.

PD-089828 Chemical Structure

PD-089828 Chemical Structure

CAS No. : 179343-17-0

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Description

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD 089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro[1].

IC50 & Target[1]

FGFR1

0.15 μM (IC50)

PDGFR-β

1.76 μM (IC50)

EGFR

5.47 μM (IC50)

c-Src

0.18 μM (IC50)

In Vitro

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC50 of 0.82 µM[1].
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC50 value of 10.9 µM[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50 value of 0.63 µM[1]. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM[1].
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[1].

Cell Proliferation Assay[1]

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[1]

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 IC50 of 0.82 µM.
Molecular Weight

405.28

Formula

C₁₈H₁₈Cl₂N₆O

CAS No.

179343-17-0

SMILES

O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PD-089828PD089828PD 089828FGFRPDGFREGFRSrcFibroblast growth factor receptorPlatelet-derived growth factor receptorEpidermal growth factor receptorErbB-1HER1ATPcompetitiveautophosphorylationphosphorylationvascularsmoothmusclecellsnonselectiveantiproliferativeantimigratoryInhibitorinhibitorinhibit

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