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Merck

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

Product Name

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.

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

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

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.

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.

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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