货号 | 10010177-500ug |
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 PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively.5 It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 µM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.5 |
别名 | PI3Kα Inhibitor 2;Phosphatidylinositol 3-Kinase α Inhibitor 2; |
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.Hayakawa, M.,Kaizawa, H.,Moritomo, H., et al. Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors. Bioorganic & Medicinal Chemistry 14, 3847-6858 (2006). | |
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 | 313.4 |
分子式 | C16H15N3O2S |
CAS号 | 371943-05-4 |
稳定性 | ≥ 2 years |
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