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Merck

658552

Tyrphostin AG 1478

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

Sinónimos:

AG 1478, 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline

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Fórmula empírica (notación de Hill):
C16H14ClN3O2
Número CAS:
175178-82-2
Peso molecular:
315.75
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00270914

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Nombre del producto

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.

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

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

Quality Level

100

Categorías relacionadas

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

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.

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

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.

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.

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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