| 货号 | 14567-1mg |
| 描述 | Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.1,2 PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).3,4 It is active both in vitroandin vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.3,4 PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).5 PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.6,7 |
| 别名 | PK-1587;PKI-587; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Petroulakis, E.,Mamane, Y.,Le Bacquer, O., et al. mTOR signaling: implications for cancer and anticancer therapy. British Journal of Cancer 94, 195-199 (2006). 2.Liu, P.,Cheng, H.,Roberts, T.M., et al. Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer. Nature Reviews.Drug Discovery 8(8), 627-644 (2009). 3.Mallon, R.,Feldberg, L.R.,Lucas, J., et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clinical Cancer Research 17(10), 3193-3203 (2011). 4.Venkatesan, A.M.,Dehnhardt, C.M.,Delos Santos, E., et al. Bis(morpholino-1,3,5-triazine) derivatives: Potent adenosine 5-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. Journal of Medicinal Chemistry 53(6), 2636-2645 (2010). 5.Gedaly, R.,Galuppo, R.,Musgrave, Y., et al. PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation. Journal of Surgical Research 185(1), 225-230 (2013). 6.DAmato, V.,Rosa, R.,DAmato, C., et al. The dual PI3K/mTOR inhibitor PKI-587 enhances sensitivity to cetuximab in EGFR-resistant human head and neck cancer models. British Journal of Cancer 110(12), 2887-2895 (2014). 7.Leiker, A.J.,DeGraff, W.,Choudhuri, R., et al. Radiation enhancement of head and neck squamous cell carcinoma by the dual PI3K/mTOR inhibitor PF-05212384. Clinical Cancer Research 21, 2792-2801 (2015). | |
| 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 | 615.7 |
| 分子式 | C32H41N9O4 |
| CAS号 | 1197160-78-3 |
| 稳定性 | ≥ 2 years |
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