產(chǎn)品說(shuō)明
REGFR抑制劑
該產(chǎn)品包含在以下化合物庫(kù)中:
- Bioactive Compound Library
- JAK/STAT Compound Library
質(zhì)量控制
化學(xué)性質(zhì)
CAS號(hào) | 171745-13-4 | ? | ? |
別名 |
分子式 | C18H18BrN3O2 | 分子量 | 388.3 |
溶解性 | >16.95mg/mL in DMSO | 儲(chǔ)存條件 | Store at -20° |
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實(shí)驗(yàn)操作
細(xì)胞實(shí)驗(yàn)[2]: |
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動(dòng)物實(shí)驗(yàn)[3]: |
動(dòng)物模型 | |
劑量 | |
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References: |
產(chǎn)品描述
Compound 56,4-[(3-溴苯基)氨基]-6,7-二乙氧基喹唑啉,是表皮生長(zhǎng)因子受體酪氨酸激酶有效的、特定的抑制劑(IC50 = 0.006 nM)。它競(jìng)爭(zhēng)性結(jié)合表皮生長(zhǎng)因子受體的三磷酸腺苷(ATP)位點(diǎn)。Compound 56能夠抑制EGF依賴性的表皮生長(zhǎng)因子受體的磷酸化、抑制表皮生長(zhǎng)因子受體過表達(dá)人類癌細(xì)胞株系的增殖和平板的集落生成,并在成纖維細(xì)胞過表達(dá)表皮生長(zhǎng)因子受體中阻止EGF調(diào)節(jié)的有絲分裂和致癌轉(zhuǎn)換,它還能輕微地抑制人類表皮生長(zhǎng)因子受體2(HER2/neu)的酪氨酸激酶。
參考文獻(xiàn):
[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.
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