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Merck
CN

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:
71897-07-9
Molecular Weight:
234.30
MDL number:
MFCD00270912
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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SMILES string

n1c2c(ncc1c3ccccc3)cc(c(c2)C)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

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

Quality Level

100

Related Categories

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
Product competes with ATP.
Reversible: yes
Target IC50: 500 nM against PDGFR kinase

Preparation Note

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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