| 货号 | 13873-1mg |
| 描述 | SU 6668 is an inhibitor of the receptor tyrosine kinases PDGFRβ, VEGFR2, and FGFR1 (IC50 = 0.06, 2.4, and 3.0 μM, respectively) but not EGFR (IC50 >100 μM).1,2 Through these actions, SU 6668 suppresses tumor growth, blocks angiogenesis in tumors, and induces apoptosis of tumor vasculature and regression of established tumors.3,4,5 It also inhibits metastasis in a mouse orthotopic model of melanoma.6 SU 6668 also inhibits Aurora kinases B and C (IC50 = 35 and 210 nM, respectively) and may target other kinases.7,8 |
| 别名 | NSC 702827;Orantinib;TSU-68; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sun, L.,Tran, N.,Liang, C., et al. Design, synthesis, and evalutaions of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. Journal of Medicinal Chemistry 42, 5120-5130 (1999). 2.Kammasud, N.,Boonyarat, C.,Sanphanya, K., et al. 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorganic & Medicinal Chemistry Letters 19(3), 745-750 (2009). 3.Laird, A.D.,Vajkoczy, P.,Shawver, L.K., et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Research 60, 4152-4160 (2000). 4.Griffin, R.J.,Williams, B.W.,Wild, R., et al. Simultaneous inhibition of the receptor kinase activity of vascular endothelial, fibroblast, and platelet-derived growth factors suppresses tumor growth and enhances tumor radiation response. Cancer Research 62, 1702-1706 (2002). 5.Laird, A.D.,Christensen, J.G.,Li, G., et al. SU6668 inhibits Flk-1/KDR and PDGFRβ in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. The FASEB Journal 16, 681-690 (2002). 6.Gangjee, A.,Kurup, S.,Ihnat, M.A., et al. Synthesis and biological activity of N4-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. Bioorganic & Medicinal Chemistry 18(10), 3575-3587 (2010). 7.Godl, K.,Gruss, O.J.,Eickhoff, J., et al. Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling. Cancer Research 65(15), 6919-6926 (2005). 8.Bain, J.,Plater, L.,Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochemistry Journal 408, 297-315 (2007). | |
| 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 | 310.4 |
| 分子式 | C18H18N2O3 |
| CAS号 | 252916-29-3 |
| 稳定性 | ≥ 2 years |
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