658551

AG 1296

A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors and β-receptors.

• Synonyme(s) : AG 1296, 6,7-Dimethoxy-3-phenylquinoxaline
• Formule empirique (notation de Hill): C₁₆H₁₄N₂O₂
• Numéro CAS: 146535-11-7
• Poids moléculaire : 266.29
• Numéro MDL: MFCD00270913
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 10 mg/mL; acetonitrile: soluble
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
• Clé InChI: QNOXYUNHIGOWNY-UHFFFAOYSA-N

Description

Description générale

Similar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC₅₀ = 1.0 µM) and β-receptors (IC₅₀ = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60^c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC₅₀ of 300 nM and ~1 µM, respectively.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Autres remarques

Tse, KF., et al. 2002. Leukemia16, 2027.
Tse, KF., et al. 2001. Leukemia15, 1001.
Strutz, F., et al. 2001. Kidney Int.59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3