产品说明书
NVP-TAE 226
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同义名 : | TAE226 |
| CAS号 : | 761437-28-9 | |
| 货号 : | A121000 | |
| 分子式 : | C23H25ClN6O3 | |
| 纯度 : | 98+% | |
| 分子量 : | 468.936 | |
| MDL号 : | MFCD12031516 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 10 mg/mL(21.32 mM)，配合低频超声，并水浴加热至45℃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 |
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| 动物实验配方： |
0.5% methylcellulose+water 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Both abnormal activity of FAK (focal adhesion kinase) and IGF-IR (Insulin-like growth factor-I receptor) contribute to highly infiltrative and rapid growth characteristics in tumors, as FAK can regulate tumor migration, while the expression of IGF-IR correlate with tumor grade and involved in proliferation and survival. NVP-TAE 226 is multiple-target tyrosine kinase inhibitor with IC50 of 5.5nM and 120-160nM for FAK and IGF-IR (measured by in vitro kinase assays), respectively. Treatment with NVP-TAE 226 at concentration of 0.25-1μM could dose-dependently inhibit extracellular matrix (ECM)–induced activation of FAK on its Tyr397 phosphorylation site, as well as IGF-1-induced activation of IGF-1/AKT signaling, shown as decreased p-IGF1R, p-AKT and p-ERK, in U87 cells. Also NVP-TAE 226 significant inhibited glioma cell growth and disrupted cell cycle distribution with a marked decline in cyclin B1 and p-cdc2 protein expression at concentration of 10μM, as well as induces apoptosis in glioma cells containing mut-p53 at concentration of 1μM, including U251, LN18 and LN229 cell lines. As prediction, inhibition of FAK by 1μM NVP-TAE 226 significantly decreased the invasive propensity of glioma cells U87, U87/EGFRvIII, U251, and LN18. Oral administration of NVP-TAE 226 at dose of 50mg/kg and 75mg/kg prolonged the survial of prolongs the survival of glioma cell LN229 xenograft animals[1]. | ||
| 作用机制 | NVP-TAE 226 is a potent ATP-competitive inhibitor of several tyrosine protein kinases.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| BT474 cells | 1 μM | Function assay | 24 h | Induction of apoptosis in human BT474 cells assessed as cleavage of 89 kDa PARP at 1 uM after 24 hrs by Western blotting | 18989950 |
| HCT116 cells | Proliferation assay | 48 h | Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay, IC50=0.4 μM | 25180654 | |
| HUVEC | Function assay | 72 h | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay, IC50=1 μM | 23845217 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.66mL 2.13mL 1.07mL |
21.32mL 4.26mL 2.13mL |
