658552
Tyrphostin AG 1478
≥98% (HPLC), epidermal growth factor receptor kinase inhibitor, solid
别名:
AG 1478, 4-(3-氯苯胺)-6,7-二甲氧基喹唑啉
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关于此项目
经验公式（希尔记法）:
C16H14ClN3O2
化学文摘社编号:
分子量:
315.75
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
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.
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
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
细胞可渗透性：是
可逆性：是
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。
靶标IC50：3 nM，针对表皮生长因子受体激酶
Disclaimer
毒性：标准处理（A）
General description
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）。
Legal Information
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
Other Notes
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.
Preparation Note
仅在使用前再用水相缓冲液进行稀释。
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
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