179343-17-0

179343-17-0 structure

Name: PD-089828
Chemical Name: 1-[2-amino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
CAS Number: 179343-17-0
Molecular Formula: C₁₈H₁₈Cl₂N₆O
Molecular Weight: 405.28100
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2017-05-18 13:25:15
Modify Date: 2024-01-11 08:32:42
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].

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

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	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
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.

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

Hazard Codes	Xi

179343-17-0	1135256-66-4
152121-53-4	1782532-06-2
199850-67-4	150527-97-2
321601-65-4	643734-74-1
929257-82-9	77422-99-2
1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1704150-89-9	1805333-47-4
1018584-77-4	1361801-40-2