PD-089828

Modify Date: 2024-01-11 08:32:42

PD-089828 Structure
PD-089828 structure
Common Name PD-089828
CAS Number 179343-17-0 Molecular Weight 405.28100
Density N/A Boiling Point N/A
Molecular Formula C18H18Cl2N6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PD-089828


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].

 Names

Name 1-[2-amino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
Synonym More Synonyms

 PD-089828 Biological Activity

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].
Related Catalog
Target

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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C18H18Cl2N6O
Molecular Weight 405.28100
Exact Mass 404.09200
PSA 105.82000
LogP 5.54590

 Safety Information

Hazard Codes Xi

 Synonyms

1-[2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
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