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Key Documents

658548

Sigma-Aldrich

AG 1478

InSolution, ≥98%, inhibitor EGF receptor tyrosine kinase

Synonym(s):

InSolution AG 1478

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About This Item

Empirical Formula (Hill Notation):
C16H14ClN3O2
CAS Number:
175178-82-2
Molecular Weight:
315.75
MDL number:
MFCD00270914
UNSPSC Code:
12352200
NACRES:
NA.32

Quality Level

100

Assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

clearfaint tan

shipped in

wet ice

storage temp.

−20°C

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

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Epidermal growth factor receptor kinase
Product competes with ATP.
Reversible: yes
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 Code

10 - Combustible liquids

WGK

WGK 2

Flash Point(F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Flash Point(C)

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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