产品说明书
Icotinib
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同义名 : | BPI-2009;BPI 2009H;Conmana |
| CAS号 : | 610798-31-7 | |
| 货号 : | A120776 | |
| 分子式 : | C22H21N3O4 | |
| 纯度 : | 98+% | |
| 分子量 : | 391.42 | |
| MDL号 : | MFCD22124501 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 150 mg/mL(383.22 mM)，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 |
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| 动物实验配方： |
0.5% CMC+water 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | The EGFR pathway is involved in angiogenesis, as well as cell proliferation and anti-apoptosis. EGFR encodes the EGFR (also known as ErbB1), a member of the ErbB family of receptor tyrosine kinases (RTKs). Other family members include HER2 (neu, ErbB2), HER3 (ErbB3), and HER4 (ErbB4). The ErbB RTKs are involved in intracellular signaling cascades that promote cell proliferation and survival, but can also drive malignant transformation[1]. Icotinib is a highly-selective epidermal growth factor receptor tyrosine kinase inhibitor with an IC50 of 5 nM[2]. Icotinib can bind reversibly to ATP's binding site on EGFR protein and thus prevent completion of the signal transduction cascade[3]. Blocking EGFRT with Icotinib treatment was sufficient to inhibit phosphorylation of Stat3 and Akt, which are key proteins in the EGFR signaling pathway, thus effectively blocking EGFR signaling pathway[4]. A431 cells were treated with the indicated concentration of Icotinib ranging from 0 to 250 nM for 2.5 h followed 100 ng/ml of EGF for 5 min before lysis. It was demonstrated that Icotinib markedly inhibited tyrosine phosphorylation of a wide range of intracellular proteins without altering the protein level of EGFR[2]. In a vivio study, oral administration of Icotinib at a dose of 60 mg/kg daily, five times per week significantly inhibited the volume of tumor in HCC827 xenograft models, in comparision with models[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.26mL |
12.77mL 2.55mL 1.28mL |
25.55mL 5.11mL 2.55mL |
| 参考文献 |
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