| 货号 | 10793-50mg |
| 描述 | Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.1 AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).2 Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.3 AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.4 |
| 别名 | Tyrphostin AG-879; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gazit, A.,Yaish, P.,Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. Journal of Medicinal Chemistry 32(10), 2344-2352 (1989). 2.Levitzki, A. and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205), 1782-1788 (1995). 3.He, H.,Hiokawa, Y.,Gazit, A., et al. The tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation. Cancer Biology and Therapy 3(1), 96-101 (2004). 4.Lee, H.K.,Seo, I.A.,Lee, S.H., et al. Tyrphostin ErbB2 inhibitors AG825 and AG879 have non-specific suppressive effects on gp130/ STAT3 signaling. Korean J.Physiol.Pharmacol. 12(5), 281-286 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 316.5 |
| 分子式 | C18H24N2OS |
| CAS号 | 148741-30-4 |
| 稳定性 | ≥ 2 years |
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