PD-089828

• CAT Number: R027607
• CAS Number: 179343-17-0
• Molecular Formula: C18H18Cl2N6O
• Molecular Weight: 405.28
• Purity: ≥95%
• Synonyms: 1-[2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
• InChI: InChI=1S/C18H18Cl2N6O/c1-18(2,3)26-17(27)25-15-10(13-11(19)5-4-6-12(13)20)7-9-8-22-16(21)24-14(9)23-15/h4-8H,1-3H3,(H4,21,22,23,24,25,26,27)
• InChIKey: RRWSNCZYJCOEFX-UHFFFAOYSA-N
• SMILES: CC(C)(C)NC(=O)NC1=C(C=C2C=NC(=NC2=N1)N)C3=C(C=CC=C3Cl)Cl

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. PD-089828 has a long-lasting cellular activity[1].
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].

Reference

[1]. Dahring TK, et al. Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. J Pharmacol Exp Ther. 1997 Jun;281(3):1446-56.
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