货号 | 4350/50 |
别名 | N-Methyl-[[3[(1E)-2-(2-pyridinyl)et |
供应商 | Tocris |
生物活性 | Potent inhibitor of VEGFR-2, -3, and -1 (IC50 values are 0.2, 0.1-0.3, and 1.2 nM respectively). Exhibits minimal activity against a panel of ~100 protein kinase. Inhibits angiogenesis and vascular permeability. Also a high affinity BCR-ABL1 (T315I) inhibitor (Ki = 149 pM for autophosphorylated ABL1 (T315I)). Blocks proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Orally available. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 386.47 |
分子式 | C22H18N4OS |
可溶性/溶解性 | Soluble to 25 mM in DMSO |
参考文献 | Pemovskaet al (2015) Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 519 102. PMID: 25686603. Hu-Loweet al (2008) Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2 and 3. Clin.Cancer Res. 14 7272. PMID: 19010843. Ma and Waxman (2008) Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 7 79. PMID: 18202011. |