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.
别名:
AG 1296, 6,7-Dimethoxy-3-phenylquinoxaline
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
InChI key
QNOXYUNHIGOWNY-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 10 mg/mL, acetonitrile: soluble
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
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 p60c-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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFR kinase
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
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
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