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
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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]. |
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| 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 |
| Molecular Formula | C18H18Cl2N6O |
|---|---|
| Molecular Weight | 405.28100 |
| Exact Mass | 404.09200 |
| PSA | 105.82000 |
| LogP | 5.54590 |
| Hazard Codes | Xi |
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