| 货号 | 13813-500mg |
| 描述 | Axitinib is a tyrosine kinase inhibitor that blocks the activation of VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ (IC50 = 1.2, 0.25, 0.29, 1.7, and 1.6 nM, respectively).1 Through its effects on VEGFRs, it causes regression of fenestrated, VEGFR-rich capillaries in tumors and normal tissue of mice, which is reversed following removal of the inhibitor.2,3,4 Axitinib has shown promise as a therapeutic in certain cancers and cancer models.5,6 |
| 别名 | AG-013736; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Giles, F.J.,Bellamy, W.T.,Estrov, Z., et al. The anti-angiogenesis agent, AG-013736, has minimal activity in elderly patients with poor prognosis acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Leukemia Research 30, 801-811 (2006). 2.Inai, T.,Mancuso, M.,Hashizume, H., et al. Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. American Journal of Pathology 165(1), 35-52 (2004). 3.Kamba, T.,Tam, B.Y.Y.,Hashizume, H., et al. VEGF-dependent plasticity of fenestrated capillaries in the normal adult microvasculature. American Journal of Physiology.Heart and Circulatory Physiology 290, H560-H576 (2006). 4.Mancuso, M.R.,Davis, R.,Norberg, S.M., et al. Rapid vascular regrowth in tumors after reversal of VEGF inhibition. Journal of Clinical Investigation 116(10), 2610-2621 (2006). 5.Wilmes, L.J.,Pallavicini, M.G.,Fleming, L.M., et al. AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging. Magnetic Resonance Imaging 25, 319-327 (2007). 6.Rini, B.I. Vascular endothelial growth factor-targeted therapy in metastatic renal cell carcinoma. Cancer 115(10 Suppl), 2306-2312 (2009). | |
| 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 | 386.5 |
| 分子式 | C22H18N4OS |
| CAS号 | 319460-85-0 |
| 稳定性 | ≥ 2 years |
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