溶解性 |
|
存贮条件 | 储存温度-20°C |
应用 | A selective PI3K inhibitor |
产品介绍 | PIK-294是一种高度选择性p110δ抑制剂,IC50为10 nM,作用于PI3Kα/β/γ效果分别低1000,49和16倍。 |
备注 | PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively. |
生化机理 | PIK-294 displays selectivity with respect to the inhibition of PI3K isoforms p110β, p110δ, and p110γ, however it is most selective for PI3Kδ (IC 50 = 490, 10, and 160 nM, respectively). PIK-294 exhibits low sensitivity to p110Yalpha; with an IC50 value of 10 μM. The m-phenol moiety of PIK-294 is able to penetrate the deep-affinity pocket of the ATP binding site, and thus increases in vitro inhibitory activity. |
别名 | 2-[[4-氨基-3-(3-羟基苯基)-1H-吡唑并[3,4-d]嘧啶-1-基]甲基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮;2-[[4-Amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone |