| CAS NO: | 118409-58-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Cas No. | 118409-58-8 |
| 别名 | 酪氨酸磷酸化抑制剂25,NSC 676484,RG-50875,Tyrphostin 25,Tyrphostin AG-82 |
| 化学名 | 2-[(3,4,5-trihydroxyphenyl)methylene]-propanedinitrile |
| Canonical SMILES | OC1=CC(/C=C(C#N)/C#N)=CC(O)=C1O |
| 分子式 | C10H6N2O3 |
| 分子量 | 202.2 |
| 溶解度 | ≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | AG-82 is a cell-permeable, reversible, and competitive inhibitor of tyrosine kinase and epidermal growth factor (EGF) receptor. Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [2]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [3]. In the human epidermoid carcinoma cell line A431, AG-82 inhibited the activity of epidermal growth factor receptor kinase with an IC50 value of 3 μM [1]. AG-82 inhibited the GTPase activity of transducin with an IC50 of 7 μM. AG-82 inhibited neuromedin B-induced phosphorylation of p125FAK (focal adhesion kinase). AG-82 blocked the induction of inducible nitric oxide synthase in glial cells and Induced apoptosis in human leukemic cell lines. References: |
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