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.

• Sinónimos: AG 1295, 6,7-Dimethyl-2-phenylquinoxaline
• Fórmula empírica (notación de Hill): C₁₆H₁₄N₂
• Número de CAS: 71897-07-9
• Peso molecular: 234.30
• Número MDL: MFCD00270912
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 10 mg/mL; dichloromethane: soluble
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C
• cadena SMILES: 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
• Clave InChI: FQNCLVJEQCJWSU-UHFFFAOYSA-N

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 500 nM against PDGFR kinase

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3