| 货号 | 14617-1mg |
| 描述 | DMXAA is a xanthene which acts as a tumor vascular disrupting agent, inducing apoptosis in tumor vascular endothelium resulting in necrosis at the tumor core.1,2 It potently activates the TANK-binding kinase 1-interferon regulatory factor 3 (TBK1/IRF3) signaling pathway in leukocytes, inducing type-I-interferon (IFN) production.3,4,5 Specifically, DMXAA activates the mitochondria- and endoplasmic reticulum-associated protein known as stimulator of interferon genes (STING), leading to TBK1/IRF3 signaling.6 DMXAA signals through mouse STING but not human STING.7 In addition, DMXAA significantly inhibits several kinases in endothelial cells, including the vascular endothelial growth factor (VEGF) receptors VEGFR1 and VEGFR2 (IC50 = 119 and 11 µM, respectively).8 |
| 别名 | ASA 404;5,6-Dimethylxanthenone-4-acetic Acid;NSC 640488;Vadimezan; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.McKeage, M.J. and Baguley, B.C. Disrupting established tumor blood vessels: An emerging therapeutic strategy for cancer. Cancer 116(8), 1859-1871 (2010). 2.Thorpe, P.E. Vascular targeting agents as cancer therapeutics. Clinical Cancer Research 10(2), 415-427 (2004). 3.Roberts, Z.J.,Goutagny, N.,Perera, P.Y., et al. The chemotherapeutic agent DMXAA potently and specifically activates the TBK1-IRF-3 signaling axis. Journal of Experimental Medicine 204(7), 1559-1569 (2007). 4.Tang, C.K.,Aoshi, T.,Jounai, N., et al. The chemotherapeutic agent DMXAA as a unique IRF3-dependent type-2 vaccine adjuvant. PLoS One 8(3), (2013). 5.Wallace, A.,LaRosa, D.F.,Kapoor, V., et al. The vascular disrupting agent, DMXAA, directly activates dendritic cells through a MyD88-independent mechanism and generates antitumor cytotoxic T lymphocytes. Cancer Research 67(114), 7011-7019 (2007). 6.Prantner, D.,Perkins, D.J.,Lai, W., et al. 5,6-Dimethylxanthenone-4-acetic acid (DMXAA) activates stimulator of interferon gene (STING)-dependent innate immune pathways and is regulated by mitochondrial membrane potential. The Journal of Biological Chemisty 287(47), 39776-39788 (2012). 7.Conlon, J.,Burdette, D.L.,Sharma, S., et al. Mouse, but not human STING, binds and signals in response to the vascular disrupting agent 5,6-dimethylxanthenone-4-acetic acid. Journal of Immunology 190(10), 5216-5225 (2013). 8.Buchanan, C.M.,Shih, J.H.,Astin, J.W., et al. DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular. Clin.Sci.(Lond) 122(10), 449-457 (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 | 282.3 |
| 分子式 | C17H14O4 |
| CAS号 | 117570-53-3 |
| 稳定性 | ≥ 2 years |
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