521234

PDGFR Tyrosine Kinase Inhibitor V

The PDGFR Tyrosine Kinase Inhibitor V, also referenced under CAS 347155-76-4, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonim(y): PDGFR Tyrosine Kinase Inhibitor V, N-(4-((6,7-Dimethoxy-4-quinoyl)oxy)phenyl)-Nʹ-(2-methylbenzoyl)thiourea, Ki11502
• Wzór empiryczny (zapis Hilla): C₂₆H₂₃N₃O₄S · 3H₂O
• Numer CAS: 347155-76-4
• Masa cząsteczkowa: 527.59
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD12032139
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: S=C(Nc2ccc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)NC(=O)c1c(cccc1)C
• InChI: 1S/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 key: ZXGIBSBJQLLUEE-UHFFFAOYSA-N

Opis

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)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable