AG-1478
产品说明书
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同义名 : | - |
| CAS号 : | 153436-53-4 | |
| 货号 : | A103804 | |
| 分子式 : | C16H14ClN3O2 | |
| 纯度 : | 99% | |
| 分子量 : | 315.75 | |
| MDL号 : | MFCD00270914 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(158.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Epidermal growth factor (EGF) is a well-known growth factor that promotes cancer progression. EGF stimulates cancer growth through the EGFR receptor (EGFR) pathway. Most of cancer tissues are shown to overexpress EGFR, and EGF-EGFR axis has been considered an attractive target for cancer treatment. Indeed, EGFR-tyrosine kinase inhibitors (EGFR-TKIs) have been developed and clinically used in patients with malignancy. EGFR-TKI effectively blocks the EGFR pathway via suppression of EGFR phosphorylation and can therefore inhibit the growth of cancer cells dramaticallyIshiguro Y, Ishiguro H, Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget. 2013 Apr;4(4):550-9. doi: 10.18632/oncotarget.939. PMID: 23592411; PMCID: PMC3720603.|https://pubmed.ncbi.nlm.nih.gov/23592411/}. The quinazoline AG 1478 have been shown to selectively inhibit EGF receptor tyrosine kinase activity in vitro as compared to a variety of tyrosine kinases, including the closely related HER-2/Neu receptor. The IC50s are 0.0020 μM, 2.6 μM, > 100 μM, and >100 μM for EGFR/HER-1 HER-2/neu Insulin-R and c-src, respectively{{Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997 Jun 30;410(2-3):187-90. doi: 10.1016/s0014-5793(97)00580-2. PMID: 9237626.|https://pubmed.ncbi.nlm.nih.gov/9237626/. In vitro study, AG1478 (1 or 10 mg/kg) was intraperitoneally injected to OVA-induced mice at 1 h before the intranasal challenge with OVA, it was showed that AG-1478 significantly and dose-dependently inhibited OVA-induced goblet cell metaplasia, mucus production and infiltration of eosinophils and neutrophils[3]. Cells were pre-treated with AG1478 antibody before EGF treatment, EGFR phosphorylation was inhibited especially in HSC-3. AG1478 also inhibited phosphorylation of STAT3, Akt, and MAPK induced by EGF. These results suggested that EGFR-TK antibody decreased cell growth via inhibiting EGF phosphorylation[4]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| A431 | ~10 μM | Kinase assay | inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR | 10702262 | |
| A431 | ~10 μM | Function assay | induces cell cycle arrest | 10702262 | |
| CNE2 | 100 μM | Growth inhibitory assay | inhibits cell proliferation by 98.4% | 11410322 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.17mL 0.63mL 0.32mL |
15.84mL 3.17mL 1.58mL |
31.67mL 6.33mL 3.17mL |
| 参考文献 |
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