| 货号 | 14868-100mg |
| 描述 | Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC50 values of 77, 37, and 190 nM, respectively.1,2 It less potently inhibits PDGF and c-Kit (IC50 = 600 and 700 nM) and has no effect on a large panel of additional kinases.1,3,2 Vatalanib completely blocks retinal neovascularization in oxygen-induced ischemic retinopathy in mice, suggesting its use in diabetic retinopathy and other diseases featuring aberrant vascular development.4,5 |
| 别名 | CGP 79787;PTK787;PTK/ZK; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bold, G.,Altmann, K.H.,Frei, J., et al. New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. Journal of Medicinal Chemistry 43(16), 3200 (2000). 2.Fabian, M.A.,Biggs, W.H., III,Treiber, D.K., et al. A small molecule-kinase interaction map for clinical kinase inhibitors. Nat.Biotechnol. 23(3), 329-336 (2005). 3.Furet, P.,Bold, G.,Hofmann, F., et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorganic & Medicinal Chemistry Letters 13(18), 2967-2971 (2003). 4.Ozaki, H.,Seo, M.S.,Ozaki, K., et al. Blockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularization. American Journal of Pathology 156(2), 697-707 (2000). 5.Giatromanolaki, A.,Koukourakis, M.,Sivridis, E., et al. Vascular density analysis in colorectal cancer patients treated with vatalanib (PTK787/ZK222584) in the randomised CONFIRM trials. British Journal of Cancer 107(7), 1044-1050 (2012). | |
| 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 | 419.7 |
| 分子式 | C20H15ClN4 • 2HCl |
| CAS号 | 212141-51-0 |
| 稳定性 | ≥ 2 years |
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