Compound 56

产品说明

该产品包含在以下化合物库中:

• Bioactive Compound Library
• JAK/STAT Compound Library

质量控制

• 纯度 = 97.00%

化学性质

实验操作

产品描述

Compound 56，4-[(3-溴苯基)氨基]-6，7-二乙氧基喹唑啉，是表皮生长因子受体酪氨酸激酶有效的、特定的抑制剂（IC50 = 0.006 nM)。它竞争性结合表皮生长因子受体的三磷酸腺苷(ATP)位点。Compound 56能够抑制EGF依赖性的表皮生长因子受体的磷酸化、抑制表皮生长因子受体过表达人类癌细胞株系的增殖和平板的集落生成，并在成纤维细胞过表达表皮生长因子受体中阻止EGF调节的有丝分裂和致癌转换，它还能轻微地抑制人类表皮生长因子受体2(HER2/neu)的酪氨酸激酶。

参考文献：
[1].  Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, and Denny WA. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.J Med Chem 1966; 39 (1): 267-276.
[2].  Monique Bos, Jhn Mendelsohn, Young-Mee Kim, Joan Albanell, David W. Fry, and Jose Baelga. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res 1997;3:2099-2106.