Vactosertib
Cat. No.：YN460029
CAS No. ：1352608-82-2
| 产品名称: | Vactosertib |
| CAS No.: | 1352608-82-2 |
| Chemical Name: | N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazole-2-methanamine |
| Synonyms: | EW-7197; TEW-7197 |
| 分子量: | 399.42 |
| 分子式: | C₂₂H₁₈FN₇ |
| SMILES: | CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)NC(CNC5=CC=CC=C5F)=N2)=N1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Vactosertib (EW-7197) 是一种有效的，具有口服活性且具有 ATP 竞争性激活素受体样激酶 5 (ALK5) 抑制剂，IC50为 12.9 nM。Vactosertib 还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM)。Vactosertib 具有强大的抗转移活性和抗癌作用。 |
| IC50和靶点: | [{name:"ALK5:12.9 nM (IC50)"}] |
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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 agentJ. Med. Chem.57(10),4213-4238(2014)
Son, J.Y., Park, S.-Y., Kim, S.-J., et al.EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasisMol. Cancer Ther.13(7),1704-1716(2014)
Kaowinn, S., Kim, J., Lee, J., et al.Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-β signalingOncotarget8(3),5092-5110(2017)
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 transitionCell Physiol. Biochem.38(2),571-588(2016)
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 lymphocytesEMBO Mol. Med.5(11),1720-1739(2013)
