658552

Tyrphostin AG 1478

≥98% (HPLC), epidermal growth factor receptor kinase inhibitor, solid

• Synonym(s): AG 1478, 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
• Empirical Formula (Hill Notation): C₁₆H₁₄ClN₃O₂
• CAS Number: 175178-82-2
• Molecular Weight: 315.75
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00270914
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Product Name: AG 1478, 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.
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: pale yellow
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: Clc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC
• InChI: 1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
• InChI key: GFNNBHLJANVSQV-UHFFFAOYSA-N

Description

General description

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.

Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Product competes with ATP.

Primary Target
Epidermal growth factor receptor kinase

Target IC₅₀: 3 nM against epidermal growth factor receptor kinase

Preparation Note

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

Further dilute with aqueous buffers just prior to use.

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3