质量水平
检测方案
≥98% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
−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 key
GFNNBHLJANVSQV-UHFFFAOYSA-N
一般描述
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
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）
制备说明
仅在使用前再用水相缓冲液进行稀释。
重悬
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.
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
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
WGK
WGK 3
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