| 货号 | 11600-100mg |
| 描述 | The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.1,2 GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.3,4 It is much less effective against class II-IV isoforms of PI3K and against mTOR.3,5 GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.3,6 |
| 别名 | GNE-0941;Pictilisib;Pictrelisib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.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). 2.Hirsch, E.,Ciraolo, E.,Ghigo, A., et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacology & Therapeutics 118, 192-205 (2008). 3.Folkes, A.J.,Ahmadi, K.,Alderton, W.K., et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. Journal of Medicinal Chemistry 51(18), 5522-5532 (2008). 4.Berndt, A.,Miller, S.,Williams, O., et al. The p110δ structure: Mechanisms for selectivity and potency of new PI(3)K inhibitors. Nature Chemical Biology 6(2), 117-124 (2010). 5.Sutherlin, D.P.,Sampath, D.,Berry, M., et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors. Journal of Medicinal Chemistry 53(3), 1086-1097 (2010). 6.Raynaud, F.I.,Eccles, S.A.,Patel, S., et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: From PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Molecular Cancer Therapeutics 8(7), 1725-1738 (2009). | |
| 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 | 513.6 |
| 分子式 | C23H27N7O3S2 |
| CAS号 | 957054-30-7 |
| 稳定性 | ≥ 2 years |
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