| 货号 | 16619-1mg |
| 描述 | TGF-β is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies.1,2 TGF-β signals through two receptor tyrosine kinases, TGF-βRI and TGF-βRII. SD 208 is a potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other tyrosine or serine/threonine kinases, including TGF-βRII kinase.3 It blocks both autocrine and paracrine TGF-β signaling in glioma cells, inhibiting TGF-β-induced migration and invasion without affecting viability or proliferation.3 SD 208 is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice.3 It improves survival in mice with xenografted glioma by heightening the immune response against tumor cells and reverses bronchial hyperresponsiveness to allergens in ovalbumin-exposed mice.3,4 SD 208 also suppresses TGF-β-induced differentiation of proliferating myofibroblasts and induces dedifferentiation in the absence of TGF-β.5,6 |
| 别名 | TGF-β RI Kinase Inhibitor V; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fuxe, J.,Vincent, T. and de Herreros, A.G. Transcriptional crosstalk between TGF-β and stem cell pathways in tumor cell invasion. Cell Cycle 9(12), 2363-2374 (2010). 2.Distler, J.H.W. and Distler, O. Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis. Rheumatology 47, 10-11 (2008). 3.Uhl, M.,Aulwurm, S.,Wischhusen, J., et al. SD-208, a novel transforming growth factor β receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Research 64(21), 7954-7961 (2004). 4.Leung, S.Y.,Niimi, A.,Noble, A., et al. Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. Journal of Pharmacology and Experimental Therapeutics 319(2), 586-594 (2006). 5.Driesen, R.B.,Nagaraju, C.K.,Abi-Char, J., et al. Reversible and irreversible differentiation of cardiac fibroblasts. Cardiovascular Research 101(3), 411-422 (2014). 6.Kapoun, A.M.,Gaspar, N.J.,Wang, Y., et al. Transforming growth factor-β receptor type 1 (TGFRI) kinase activity but not p38 activation is required for TGFRI-induced myofibroblast differentiation and profibrotic gene expression_. Molecular Pharmacology 70(2), 518-531 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 352.8 |
| 分子式 | C17H10ClFN6 |
| CAS号 | 627536-09-8 |
| 稳定性 | ≥ 2 years |
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