产品说明

一般描述

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.

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

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

警告

Toxicity: Irritant (B)

外形

A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658552) in DMSO.

重悬

Following initial thaw, aliquot and freeze (-20°C).

其他说明

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.

法律信息

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

基本信息

产品性质

安全信息

产品说明

应用

酪氨酸磷酸化抑制剂AG 1478已用作表皮生长因子受体(EGFR)酪氨酸激酶抑制剂，用于研究其在boyden小室迁移检测中对硬纤维瘤细胞迁移的影响。它还用于抑制A431表皮样癌细胞株中外源性转化生长因子α介导的磷酸化。

包装

1, 5 mg in ampule

生化/生理作用

酪氨酸磷酸化抑制剂AG 1478是一种表皮生长因子受体(EGFR)酪氨酸激酶抑制剂。它可导致大鼠的低镁血症和心功能障碍发展。酪氨酸磷酸化抑制剂AG 1478是乳腺癌的潜在治疗剂。
表皮生长因子受体蛋白选择性抑制剂

特点和优势

该化合物列于《受体分类和信号转导手册》的 EGFR 页面。要浏览其他手册页， 单击此处 。
该化合物是激酶磷酸酶生物学研究的特色产品。 点击此处 ，发现更多特色激酶磷酸酶生物学产品。在 sigma.com/discover-bsm了解更多关于其他研究领域的生物活性小分子。

制备说明

酪氨酸磷酸化抑制剂 AG 1478 溶于 DMSO：MeOH (1:1)，浓度为 10 mg/mL，得到澄清、无色溶液。也可溶于二氯甲烷 (10 mg/mL)、乙醇 (10 mg/mL) 和 0.1 NHCl(低于 0.4 mg/mL)。但不溶于水、2-羟丙基-β-环糊精和 0.1n NaOH。

基本信息

产品性质

安全信息

产品说明

一般描述

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.
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.

包装

5 mg in Plastic ampoule

生化/生理作用

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

警告

Toxicity: Standard Handling (A)

制备说明

Further dilute with aqueous buffers just prior to use.

重悬

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

其他说明

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.

法律信息

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

基本信息

产品性质

安全信息