| 货号 | 15220-50mg |
| 描述 | Dovitinib is a receptor tyrosine kinase inhibitor that targets vascular endothelial growth factor-2, basic fibroblast growth factor-1, and platelet-derived growth factor β receptors (IC50s = 65, 11, and 5 nM, respectively).1 By impairing these kinase signals, 1 μM dovitinib has been shown to prevent the growth and motility of pancreatic cancer cell lines (HPAF-II, BxPC-3, MiaPaCa2, and L3.6pl).2 At 0.04 μM, dovitinib can inhibit endothelial cell proliferation and motility.3 These antiangiogenic effects have been proposed to be the mechanism by which dovitinib inhibits hepatocellular carcinoma growth and metastasis.3 Dovitinib has been evaluated in clinical trials for the treatment of advanced solid tumors.4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Renhowe, P.A.,Pecchi, S.,Shafer, C.M., et al. Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: A novel class of receptor tyrosine kinase inhibitors. Journal of Medicinal Chemistry 52(2), 278-292 (2009). 2.Taeger, J.,Moser, C.,Hellerbrand, C., et al. Targeting FGFR/PDGFR/VEGFR impairs tumor growth, angiogenesis, and metastasis by effects on tumor cells, endothelial cells, and pericytes in pancreatic cancer. Molecular Cancer Therapeutics 10(11), 2157-2167 (2011). 3.Chen, Z.Y.,Shi, M.,Peng, L.X., et al. Dovitinib preferentially targets endothelial cells rather than cancer cells for the inhibition of hepatocellular carcinoma growth and metastasis. Journal of Translational Medicine 10, 245 (2012). 4.Kim, K.B.,Chesney, J.,Robinson, D., et al. Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma. Clinical Cancer Research 17(23), 7451-7461 (2011). 5.Sarker, D.,Molife, R.,Evans, T.R.J., et al. A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors. Clinical Cancer Research 14(7), 2075-2081 (2008). | |
| 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 | 392.4 |
| 分子式 | C21H21FN6O |
| CAS号 | 405169-16-6 |
| 稳定性 | ≥ 2 years |
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