PD 089828

SKU: orb1218611

Description

PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 μM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 μM)

Key Properties

• CAS Number: 179343-17-0
• MW: 405.28
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₈Cl₂N₆O
• SMILES: CC(C)(C)NC(=O)NC1=C(C=C2C=NC(=NC2=N1)N)C3=C(C=CC=C3Cl)Cl
• Target: EGFR
• Solubility: DMSO:2.5 mM

Bioactivity

• 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. 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 IC50 of 0.82 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PD-089828 | PD089828

Quick Database Links

Gene Symbol

EGFR