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.

• Synonim(y): AG 1295, 6,7-Dimethyl-2-phenylquinoxaline
• Wzór empiryczny (zapis Hilla): C₁₆H₁₄N₂
• Numer CAS: 71897-07-9
• Masa cząsteczkowa: 234.30
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 10 mg/mL; dichloromethane: soluble
• Warunki transportu: ambient
• temp. przechowywania: −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
• Klucz InChI: FQNCLVJEQCJWSU-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 500 nM against PDGFR kinase

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3