PDGFR Tyrosine Kinase Inhibitor V,1MG,521234-1MGCN,Sigma

销售价: ¥ 2874.63 / 件
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订货号 0BV5387
品牌型号 Sigma 521234-1MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

General description

A cell-permeable quinolinyl-thiourea compound that acts a potent, ATP-competitive, and reversible inhibitor of PDGFR (IC50 = 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively). Inhibits c-kit receptor only at much higher concentrations (IC50 = 434 and 234 nM in receptor phosphorylation and kinase activity, respectively). Shown to potently inhibit neointima formation in a rat carotid artery balloon injury model in vivo (30 mg/kg, p.o.).


Biochem/physiol Actions

Cell permeable: yes
Primary Target
PDGFR
Product competes with ATP.
Reversible: yes
Target IC50: 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively


Packaging

Packaged under inert gas


Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.


Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Getachew, R., et al. 2009. Eur. J. Pharmacol. In press.
Nishioka, C., et al. 2008. Blood111, 5086.
Furuta, T., et al. 2006. J. Med. Chem.49, 2186.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Toxic (F)


技术参数 Specifications
Quality Segment100
assay≥95% (HPLC)
formsolid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,protect from light
color off-white
solubilityDMSO: 25 mg/mL
shipped inambient
storage temp.2-8°C
SMILES stringS=C(Nc2ccc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)NC(=O)c1c(cccc1)C
InChI1S/C26H23N3O4S/c1-16-6-4-5-7-19(16)25(30)29-26(34)28-17-8-10-18(11-9-17)33-22-12-13-27-21-15-24(32-3)23(31-2)14-20(21)22/h4-15H,1-3H3,(H2,28,29,30,34)
InChI keyZXGIBSBJQLLUEE-UHFFFAOYSA-N
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