InSolution AG 1478 - CAS 175178-82-2 - Calbiochem

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Epidermal growth factor receptor kinase

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

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).

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.

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