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PD 089828 Sale

(Synonyms: EGF/FGF/PDGF Receptor Tyrosine Kinase Inhibitor) 目录号 : GC44583

An inhibitor of EGFR, PDGFβ, FGF, and c-Src

PD 089828 Chemical Structure

Cas No.:179343-17-0

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500μg
¥420.00
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1mg
¥805.00
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5mg
¥3,365.00
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产品描述

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). It is selective for these targets over insulin receptor tyrosine kinase, PKC, and CDK4 (IC50s = >50 µM) but does inhibit MAPK (IC50 = 7.1 µM). PD 089828 decreases PDGF-BB-, EGF-, and bFGF-induced phosphorylation of PDGFR, EGFR, and FGFR1, respectively, in a concentration-dependent manner in vitro. It also decreases serum-stimulated growth (IC50 = 1.8 µM after 8 days) and migration (IC50 = 4.5 µM) of rat aortic smooth muscle cells.

Chemical Properties

Cas No. 179343-17-0 SDF
别名 EGF/FGF/PDGF Receptor Tyrosine Kinase Inhibitor
Canonical SMILES NC(N=C1)=NC(C1=C2)=NC(NC(NC(C)(C)C)=O)=C2C3=C(Cl)C=CC=C3Cl
分子式 C18H18Cl2N6O 分子量 405.3
溶解度 DMSO: 25 mg/ml,Ethanol: 1 mg/ml 储存条件 Store at -20°C
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1 mM 2.4673 mL 12.3365 mL 24.6731 mL
5 mM 0.4935 mL 2.4673 mL 4.9346 mL
10 mM 0.2467 mL 1.2337 mL 2.4673 mL
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Research Update

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.PMID:9190882doi

PD 089828, a novel protein tyrosine kinase inhibitor of a new structural class, the 6-aryl-pyrido-[2,3-d]pyrimidines, was identified by screening a compound library with assays that measured protein tyrosine kinase activity. PD 089828 was found to inhibit human full-length fibroblast growth factor (FGF) receptor-1 (FGFR-1), platelet-derived growth factor (PDGF) receptor beta subunit (PDGFR-beta), Src nonreceptor tyrosine kinase (c-Src) and epidermal growth factor (EGF) receptor (EGFR) tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 0.15 +/- 0.02 (n = 4), 0.18 +/- 0.04 (n = 3), 1.76 +/- 0.28 (n = 4) and 5.47 +/- 0.78 (n = 6) microM, respectively. PD 089828 was further characterized as an ATP competitive inhibitor of the growth factor receptor tyrosine kinases (FGFR-1, PDGFR-beta and EGFR) but a noncompetitive inhibitor of c-Src tyrosine kinase with respect to ATP. In addition, PD 089828 inhibited PDGF- and EGF-stimulated receptor autophosphorylation in vascular SMC (VSMC) and basic FGF-mediated tyrosine phosphorylation in A121 cells with IC50 values similar to the potencies observed for inhibition of receptor tyrosine kinase activity. The inhibition of PDGF receptor autophosphorylation in VSMC by PD 089828 occurred rapidly, with maximal effects reached within 5 min of drug exposure. Inhibition after single exposure was long lasting but also rapidly reversible, occurring within 5 min after drug removal. The PDGF-induced association of downstream signaling proteins, including phosphoinositide-3-kinase (PI-3K), growth factor receptor binding protein-2 (GRB2), SH-2 domain and collagen like (Shc) and phospholipase Cgamma (PLCgamma), with VSMC PDGF receptors was also blocked as a result of the inhibition of PDGF-stimulated receptor autophosphorylation by PD 089828. PD 089828 also inhibited the PDGF-induced tyrosine phosphorylation of the 44- and 42-kDa mitogen-activated protein kinase isoforms. Moreover, the effects of PD 089828 were demonstrated in functional assays in which PDGF-stimulated DNA synthesis, PDGF-directed migration and serum-stimulated growth of VSMC were all inhibited to the same extent as PDGF receptor autophosphorylation (IC50 = 0.8, 4.5 and 1.8 microM, respectively). These results highlight the biological characteristics of PD 089828 as a novel, broadly active protein tyrosine kinase inhibitor with long-lasting but reversible cellular effects. The potential therapeutic use of these broadly acting, nonselective inhibitors as antiproliferative and antimigratory agents could extend to such diseases as cancer, atherosclerosis and restenosis in which redundancies in growth-signaling pathways are known to exist.