Tyrphostin AG 1478

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.

Reversible: yes

Cell permeable: yes

Product competes with ATP.

Primary Target
Epidermal growth factor receptor kinase

Target IC₅₀: 3 nM against epidermal growth factor receptor kinase

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

Further dilute with aqueous buffers just prior to use.

Pan, H., et al. 2008. J. Biol. Chem.283, In press.
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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.

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

Toxicity: Standard Handling (A)