| 货号 | 19231-10mg |
| 描述 | EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM).1,2 It also inhibits ALK2 and ALK4 at nanomolar concentrations.2 EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice.2 It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells.2 EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.3,4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jin, C.H.,Krishnaiah, M.,Sreenu, D., et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J. Med. Chem. 57(10), 4213-4238 (2014). 2.Son, J.Y.,Park, S.-Y.,Kim, S.-J., et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol. Cancer Ther. 13(7), 1704-1716 (2014). 3.Kaowinn, S.,Kim, J.,Lee, J., et al. Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-β signaling. Oncotarget 8(3), 5092-5110 (2017). 4.Kim, M.-J.,Park, S.-A.,Kim, C.H., et al. TGF-β type I receptor kinase inhibitor EW-7197 suppresses cholestatic liver fibrosis by inhibiting HIF1α-induced epithelial mesenchymal transition. Cell Physiol. Biochem. 38(2), 571-588 (2016). 5.Yoon, J.-H.,Jung, S.M.,Park, S.H., et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol. Med. 5(11), 1720-1739 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 399.4 |
| 分子式 | C22H18FN7 |
| CAS号 | 1352608-82-2 |
| 稳定性 | ≥ 2 years |
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