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 p210Bcr-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.
1 mg in Plastic ampoule
Packaged under inert gas
Epidermal growth factor receptor kinase
Cell permeable: yes
Product competes with ATP.
Target IC50: 3 nM against of epidermal growth factor receptor kinase
Toxicity: Irritant (B)
A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658552) in DMSO.
Following initial thaw, aliquot and freeze (-20°C).
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.
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