| 货号 | 13645-10mg |
| 描述 | PX 866 is a ring-opened analog of wortmannin (Item No. 10010591) that potently and irreversibly inhibits PI3K (IC50 = 0.1-88 nM).1,2 It less potently blocks the activity of mammalian target of rapamycin (mTOR, IC50 = 3.1 µM).2 PX 866 exhibits single agent in vivo anti-tumor activity and increases the anti-tumor effects of cisplatin and radiation treatment.1,3 In cancer cells grown in three-dimensional cultures, PX 866 reduces cell growth and motility without causing cytotoxicity.4 Consistent with having cytostatic effects, PX 866 dosing is associated with prolonged stable disease in cancer patients.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ihle, N.T.,Williams, R.,Chow, S., et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling. Molecular Cancer Therapeutics 3(7), 763-772 (2004). 2.Zask, A.,Kaplan, J.,Toral-Barza, L., et al. Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: Potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. Journal of Medicinal Chemistry 51, 1319-1323 (2008). 3.Ihle, N.T.,Paine-Murrieta, G.,Berggren, M.I., et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Molecular Cancer Therapeutics 4(9), 1349-1357 (2005). 4.Howes, A.L.,Chiang, G.G.,Lang, E.S., et al. The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures. Molecular Cancer Therapeutics 6(9), 2505-2514 (2007). 5.Hong, D.S.,Bowles, D.W.,Falchook, G.S., et al. A Multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors. Clinical Cancer Research 18(15), 4173-4182 (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 | 525.6 |
| 分子式 | C29H35NO8 |
| CAS号 | 502632-66-8 |
| 稳定性 | ≥ 2 years |
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