658552

AG 1478

A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase versus HER2-neu and platelet-derived growth factor receptor kinase.

• Synonim(y): AG 1478, 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
• Wzór empiryczny (zapis Hilla): C₁₆H₁₄ClN₃O₂
• Numer CAS: 175178-82-2
• Masa cząsteczkowa: 315.75
• Numer MDL: MFCD00270914
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: pale yellow
• rozpuszczalność: DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• ciąg SMILES: Clc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC
• InChI: 1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
• Klucz InChI: GFNNBHLJANVSQV-UHFFFAOYSA-N

Opis

Opis ogólny

A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase (IC₅₀ = 3 nM) versus HER2-neu (IC₅₀ >100 µM) and platelet-derived growth factor receptor kinase (IC₅₀ >100 µM). Abolishes MAP kinase (ERK) activation induced by Angiotensin II (Cat. No. 05-23-0101). Also inhibits the activation of EGFR kinase and MAP kinase by 4-hydroxynonenal. Downregulates ARF1 activity and disperses Golgi structure. A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658548) in DMSO is also available.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Epidermal growth factor receptor kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 3 nM against epidermal growth factor receptor kinase

Ostrzeżenie

Toxicity: Standard Handling (A)

Uwaga dotycząca przygotowania

Further dilute with aqueous buffers just prior to use.

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Inne uwagi

Pan, H., et al. 2008. J. Biol. Chem.283, In press.
Liu, W., et al. 1999. J. Cell Sci.112, 2409.
Eguchi, S., et al. 1998. J. Biol. Chem. 273, 8890.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Fry, D.W., et al. 1994. Science265, 1093.
Osherov, N., and Levitski, A. 1994. Eur. J. Biochem.225, 1047.
Ward, W.H., et al. 1994. Biochem. Pharmacol.48, 659.

Informacje prawne

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.

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

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

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