AZD3458 是一种有效的选择性 PI3Kγ 抑制剂,抑制 PI3Kγ, PI3Kα, PI3Kβ, 和 PI3Kδ,pIC50 分别为 9.1, 5.1,<4.5, 和 6.5。
PI3Kγ 9.1(pIC50) | PI3Kα 5.1(pIC50) |
PI3Kβ 4.5(pIC50) | PI3Kδ 6.5(pIC50) |
产品描述 | AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1,<4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively[1]. AZD3458 (Compound 15) also inhibits PI3KC2α, PI3KC2β, PI3KC2γ, and PI3KC3 with pIC50s of<5, 7.5, 5.5, and 5.1, respectively[1]. [1]. Pemberton N, et al. Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors. J Med Chem. 2018 Jun 28;61(12):5435-5441. |