| 货号 | 10007707-1mg |
| 描述 | Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1,2,3 PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits4 AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.5 It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.5 AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg. |
| 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.Camps, M.,Rückle, T.,Ji, H., et al. Blockade of PI3K g suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nature Medicine 11(9), 936-943 (2005). | |
| 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 | 257.3 |
| 分子式 | C12H7N3O2S |
| CAS号 | 648450-29-7 |
| 稳定性 | ≥ 2 years |
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