658550
AG 1295
A cell-permeable, reversible, ATP-competitive, and selective inhibitor of platelet-derived growth factor (PDGF) receptor kinase (IC₅₀ = 500 nM) and PDGF-dependent DNA synthesis (IC₅₀ = 2.5 µM) in Swiss/3T3 cells.
Synonym(s):
AG 1295, 6,7-Dimethyl-2-phenylquinoxaline
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About This Item
Empirical Formula (Hill Notation):
C16H14N2
CAS Number:
Molecular Weight:
234.30
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 10 mg/mL
dichloromethane: soluble
shipped in
ambient
storage temp.
−20°C
InChI
1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3
InChI key
FQNCLVJEQCJWSU-UHFFFAOYSA-N
General description
A cell-permeable, reversible, ATP-competitive, and selective inhibitor of platelet-derived growth factor (PDGF) receptor kinase (IC50 = 500 nM) and PDGF-dependent DNA synthesis (IC50 = 2.5 µM) in Swiss/3T3 cells. Has no effect on EGF receptor autophosphorylation and shows only a weak effect on EGF- or insulin-stimulated DNA synthesis. A potent blocker of smooth muscle cell proliferation.
Selectively inhibits platelet-derived growth factor (PDGF) receptor kinase (IC50 = 500 nM) and the PDGF-dependent DNA synthesis (IC50 = 2.5 µM) in Swiss 3T3 cells. Has no effect on epidermal growth factor (EGF) receptor autophosphorylation and shows only a weak effect on EGF- or insulin-stimulated DNA synthesis.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFR kinase
PDGFR kinase
Product competes with ATP.
Reversible: yes
Target IC50: 500 nM against PDGFR kinase
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Banai, S., et al. 1998. Circulation 97, 1960.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Kovalenko, M., et al. 1994. Cancer Res.54, 6106.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Kovalenko, M., et al. 1994. Cancer Res.54, 6106.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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