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About This Item
Empirical Formula (Hill Notation):
C16H14ClN3O2
CAS Number:
Molecular Weight:
315.75
UNSPSC Code:
12352200
NACRES:
NA.32
MDL number:
Assay:
≥98% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
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
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
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
Physical form
A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658552) in DMSO.
Preparation Note
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.
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: Irritant (B)
Storage Class
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)
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