| 货号 | 15250-1mg |
| 描述 | Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3 hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1,2,3 PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit.4 AZD6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).5 It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.5 AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.5,6,7 AZD6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.5 It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.8 |
| 别名 | KIN-193; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rameh, L.E. and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. The Journal of Biological Chemisty 274, 8347-8350 (1999). 2.Vivanco, I. and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews.Cancer 2, 489-501 (2002). 3.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005). 4.Rückle, T.,Schwarz, M.K. and Rommel, C. PI3Kγ inhibition: Towards an aspirin of the 21st century? Nature Reviews.Drug Discovery 5, 903-918 (2006). 5.Ni, J.,Liu, Q.,Xie, S., et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2(5), 425-433 (2012). 6.Weigelt, B.,Warne, P.H.,Lambros, M.B., et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clinical Cancer Research 19(13), 3533-3544 (2013). 7.Nichols, A.C.,Black, M.,Yoo, J., et al. Exploiting high-throughput cell line drug screening studies to identify candidate therapeutic agents in head and neck cancer. BMC Pharmacol.Toxicol. 15, (2014). 8.Nylander, S.,Kull, B.,Björkman, J.A., et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: Effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J.Thromb.Haemost. 10(10), 2127-2136 (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 | 408.5 |
| 分子式 | C22H24N4O4 |
| CAS号 | 1173900-33-8 |
| 稳定性 | ≥ 2 years |
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