AG 1478 - CAS 175178-82-2 - Calbiochem

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.

AG 1478 - CAS 175178-82-2 - Calbiochem, 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
Empirical Formula (Hill Notation):
CAS Number:
Molecular Weight:
MDL number:

storage conditions


Quality Level


≥98% (HPLC)





storage condition

OK to freeze
protect from light


pale yellow


DMSO: 5 mg/mL

shipped in


storage temp.


General description

A cell-permeable, reversible, ATP-competitive, 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. Downregulates ARF1 activity and disperses Golgi structure.
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.


5 mg in Plastic ampoule

Biochem/physiol Actions

Primary Target
Epidermal growth factor receptor kinase
Reversible: yes
Cell permeable: yes
Product competes with ATP.
Target IC50: 3 nM against epidermal growth factor receptor kinase


Toxicity: Standard Handling (A)

Preparation Note

Further dilute with aqueous buffers just prior to use.


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

Other Notes

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.

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

WGK Germany


Certificate of Analysis

Certificate of Origin

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