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(e): AG 1295, 6,7-Dimethyl-2-phenylquinoxaline
• Empirische Formel (Hill-System): C₁₆H₁₄N₂
• CAS-Nummer: 71897-07-9
• Molekulargewicht: 234.30
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 10 mg/mL; dichloromethane: soluble
• Versandbedingung: ambient
• Lagertemp.: −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
• InChIKey: FQNCLVJEQCJWSU-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 500 nM against PDGFR kinase

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3