Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetEpidermal growth factor receptor kinase

Cell permeable: yes

Target IC₅₀: 3 nM against of epidermal growth factor receptor kinase

General description

Highly potent and specific inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (IC₅₀ = 3 nM). Much higher concentrations are required for inhibition of the kinase activity of the closely related HER2 (neu/erb-B2) receptor (IC₅₀ >100 µM), the platelet-derived growth factor (PDGF) receptor (IC₅₀ >100 µM), and p210^Bcr-Abl (IC₅₀ >50 µM). Its mechanism of inhibition likely mimics that of the related compound, 4-(3-chloroanilino)quinazoline (CAQ), a competitive inhibitor with respect to ATP.

Legal Information

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

Other Notes

Levitski, 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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658552) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Irritant (B)