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Merck
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文件

658552

Sigma-Aldrich

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.

别名:

AG 1478, 4-(3-氯苯胺)-6,7-二甲氧基喹唑啉

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About This Item

经验公式（希尔记法）:
C16H14ClN3O2
CAS号:
175178-82-2
分子量:
315.75
MDL號碼:
MFCD00270914
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

solid

製造商／商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

pale yellow

溶解度

DMSO: 5 mg/mL

運輸包裝

ambient

儲存溫度

−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 密鑰

GFNNBHLJANVSQV-UHFFFAOYSA-N

一般說明

一种表皮生长因子（EGF）受体酪氨酸激酶（IC50 = 3 nM）的细胞渗透性、可逆性、ATP竞争性、高效和特异性抑制剂。抑制密切相关的HER2（neu/erb-B2）受体（IC50 >100 µM）、血小板衍生生长因子（PDGF）受体（IC50 >100 µM）和p210Bcr-Abl（IC50 >50 µM）的激酶活性需要更高的浓度。其抑制机制可能与相关化合物4-（3-氯苯胺基）喹唑啉（CAQ）相似，后者是一种与ATP有关的竞争性抑制剂。下调ARF1活性并分散高尔基体结构。
表皮生长因子受体激酶（IC50 = 3 nM）与HER2 neu（IC50 >100 µM）和血小板衍生生长因子受体激酶（IC50 >100 µM）相比，是一种细胞渗透性、可逆性、ATP竞争性、高效和选择性的抑制剂。消除血管紧张素II（目录号05-23-0101）诱导的MAP激酶（ERK）激活。还可抑制4-羟基壬烯醛对EGFR激酶和MAP激酶的激活。下调ARF1活性并分散高尔基体结构。也可购买10 mM（1 mg/317 µl）AG 1478的DMSO溶液（目录号658548）。

生化／生理作用

主要靶标
表皮生长因子受体激酶
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：3 nM，针对表皮生长因子受体激酶

警告

毒性：标准处理（A）

準備報告

仅在使用前再用水相缓冲液进行稀释。

重構

复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。

其他說明

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.

法律資訊

根据美国专利号5,457,105和欧洲专利号0,566,266的许可证销售。
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

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