Tyrphostin AG 1478

• 产品编号：CST-9842S      品牌：CST       原厂货号：9842S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

酪氨酸磷酸化抑制剂AG1478以400μg干粉形式供应。存储于-20ºC或更低的温度下。使用前，将干粉溶解于1.23 ml DMSO中制备成1 mM酪氨酸磷酸化抑制剂AG1478储备溶液。将DMSO存储液按1:10,000 或 1:5,000比例稀释，配置成工作浓度为100 nM-200 nM的工作液。根据需求的浓度处理细胞30分钟。酪氨酸磷酸化抑制剂AG1478在干粉状态下更为稳定；因此建议尽量在使用前溶解。将溶液保存于-20ºC或者更低。酪氨酸磷酸化抑制剂AG1478是一种特别选择性抑制EGFR (ErbB1)的酪氨酸激酶抑制剂，体外实验中，IC50值为3 nM(1,2)。用50-150 nM酪氨酸磷酸化抑制剂AG1478处理细胞可以充分阻断EGFR在体内的激活(3)。除了EGFR, AG 1478还能够抑制癌细胞因辐射引起的ErbB4激活(4)。AG 1478无论是单独使用，还是联合其他处理方式，在评价其抗肿瘤和抗纤维化的效果中都表现出不错的应用前景。

1. Osherov, N. and Levitzki, A. (1994) Eur J Biochem 225, 1047-53.
2. Levitzki, A. and Gazit, A. (1995) Science 267, 1782-8.
3. Fan, Z. et al. (1995) J Cell Biol 131, 235-42.
4. Bowers, G. et al. (2001) Oncogene 20, 1388-97.
5. Nagane, M. et al. (2001) J Neurosurg 95, 472-9.
6. Ishii, Y. et al. (2006) Am J Respir Crit Care Med 174, 550-6.
7. Ellis, A.G. et al. (2006) Biochem Pharmacol 71, 1422-34.
8. Rahman, M. et al. (2009) Breast Cancer Res Treat 113, 217-30.

原厂资料：

Directions for Use

Tyrphostin AG 1478 is supplied as 400 μg powder. Store at or below -20ºC. Before use, dissolve powder in 1.23 ml DMSO to make a 1 mM 
 Tyrphostin AG 1478 stock solution. For working concentrations of 100 nM-200 nM, dilute DMSO stock 1:10,000 to 1:5,000. Treat cells with the desired concentration for 30 minutes. Tyrphostin AG1478 is more stable as a powder than in solution; it is therefore recommended to dissolve as close as possible prior to use. Store solution at or below -20ºC.

Background

Tyrphostin AG 1478 is a tyrosine kinase inhibitor specifically selective to EGFR (ErbB1), with an IC50 of about 3 nM in vitro (1,2). Treatment of cell with 50-150 nM of AG 1478 can substantially block EGFR activiation in vivo (3). In addition to EGFR, AG 1478 also inhibits ErbB4 activation induced by radiation in cancer cells (4). Testing of AG 1478 alone or in combination with other treatments to assess anti-tumor and anti-fibrotic effectiveness has yielded promising results (5-8).

1. Osherov, N. and Levitzki, A. (1994) Eur J Biochem 225, 1047-53.
2. Levitzki, A. and Gazit, A. (1995) Science 267, 1782-8.
3. Fan, Z. et al. (1995) J Cell Biol 131, 235-42.
4. Bowers, G. et al. (2001) Oncogene 20, 1388-97.
5. Nagane, M. et al. (2001) J Neurosurg 95, 472-9.
6. Ishii, Y. et al. (2006) Am J Respir Crit Care Med 174, 550-6.
7. Ellis, A.G. et al. (2006) Biochem Pharmacol 71, 1422-34.
8. Rahman, M. et al. (2009) Breast Cancer Res Treat 113, 217-30.

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated.
Protect from light. In lyophilized form, the chemical is stable for
24 months. Once in solution, use within 3 months to prevent loss
of potency. Aliquot to avoid multiple freeze/thaw cycles.