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.
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
Storage Class
10 - Combustible liquids
wgk_germany
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
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