| 货号 | 16351-1mg |
| 描述 | AAL-993 is a potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively.1,2 It less potently inhibits c-Kit, colony stimulating factor 1 receptor, PGDF receptor β, and EGF receptor (IC50s = 236, 380, 640, and 1,040 nM, respectively) and is without effect on a number of other tyrosine kinases.1 AAL-993 is orally bioavailable in vivo, blocks VEGF-induced angiogenesis, and prevents the growth of primary tumors and spontaneous peripheral metastases in mice.1,3 It also inhibits hypoxia-mediated increase in hypoxia-inducible factor-1 transcriptional activity in an ERK-dependent manner (IC50 = ~5 µM).4 |
| 别名 | VEGFR Tyrosine Kinase Inhibitor VI;ZK 260253; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Manley, P.W.,Furet, P.,Bold, G., et al. Anthranilic acid amides: A novel class of antiangiogenic VEGF receptor kinase inhibitors. Journal of Medicinal Chemistry 45(26), 5687-5693 (2002). 2.Honda, T.,Tajima, H.,Kaneko, Y., et al. Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity. Bioorganic & Medicinal Chemistry Letters 18(9), 2939-2943 (2008). 3.Manley, P.W.,Bold, G.,Brüggen, J., et al. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis. Biochim.Biophys.Acta. 1697(1-2), 17-27 (2004). 4.Ban, H.S.,Uno, M. and Nakamura, H. Suppression of hypoxia-induced HIF-1α accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Letters 296(1), 17-26 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 371.4 |
| 分子式 | C20H16F3N3O |
| CAS号 | 269390-77-4 |
| 稳定性 | ≥ 2 years |
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