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658552 Sigma-AldrichAG 1478 - CAS 175178-82-2 - Calbiochem

AG 1478, CAS 175178-82-2, is a cell-permeable, potent, selective, reversible & ATP-competitive inhibitor of EGF receptor kinase (IC50 = 3 nM vs 100 µM for HER2-neu and PDGF receptor kinase).

AG 1478 - CAS 175178-82-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet
Citations

同义词: 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline

Primary Target: Epidermal growth factor receptor kinase

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
175178-82-2	C₁₆H₁₄ClN₃O₂

价格及供货情况

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Description
Overview	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.
Catalogue Number	658552
Brand Family	Calbiochem®
Synonyms	4-(3-Chloroanilino)-6,7-dimethoxyquinazoline

References
References	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. Science 267, 1782. Fry, D.W., et al. 1994. Science 265, 1093. Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047. Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.

References

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. Science 267, 1782.
Fry, D.W., et al. 1994. Science 265, 1093.
Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047.
Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.

Product Information
CAS number	175178-82-2
ATP Competitive	Y
Declaration	Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.
Form	Pale yellow solid
Hill Formula	C₁₆H₁₄ClN₃O₂
Chemical formula	C₁₆H₁₄ClN₃O₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application	AG 1478, CAS 175178-82-2, is a cell-permeable, potent, selective, reversible & ATP-competitive inhibitor of EGF receptor kinase (IC50 = 3 nM vs 100 µM for HER2-neu and PDGF receptor kinase).

Biological Information
Primary Target	Epidermal growth factor receptor kinase
Primary Target IC<sub>50</sub>	3 nM against epidermal growth factor receptor kinase
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
658552-5MGCN	07790788052232

Documentation

AG 1478 - CAS 175178-82-2 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

AG 1478 - CAS 175178-82-2 - Calbiochem 分析证书

标题	批号
658552	输入批号

参考

参考信息概述
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. Science 267, 1782. Fry, D.W., et al. 1994. Science 265, 1093. Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047. Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.

参考信息概述

引用

标题

Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.

Ying-Hong Feng, et al. (2005) Unconventional Homologous Internalization of the Angiotensin II Type-1 Receptor Induced by G-Protein-Independent Signals. Hypertension 46, 419-423.

Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	12-January-2010 RFH
Synonyms	4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
Description	A cell-permeable, reversible, ATP-competitive, 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 p210^Bcr-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. Downregulates ARF1 activity and disperses Golgi structure.
Form	Pale yellow solid
CAS number	175178-82-2
Chemical formula	C₁₆H₁₄ClN₃O₂
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (5 mg/ml). Further dilute with aqueous buffers just prior to use.
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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. Science 267, 1782. Fry, D.W., et al. 1994. Science 265, 1093. Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047. Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.
Citation	Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,. Ying-Hong Feng, et al. (2005) Unconventional Homologous Internalization of the Angiotensin II Type-1 Receptor Induced by G-Protein-Independent Signals. Hypertension 46, 419-423. Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Tyrosine Kinase (PTK) Inhibitors

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