General description
一种脂质类激酶的泛素I类PI3K(磷脂酰肌醇3-激酶)抑制剂,作用于p110α、p110β、p110δ和p110γ,IC50分别为52nM、166nM、116nM和262nM。
Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. PI3K inhibitor BKM120 specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway。
Buparlisib是泛I类磷脂酰肌醇3-激酶(PI3K)家族的具有潜在抗肿瘤活性的口服生物利用型特定口服抑制剂。 PI3K抑制剂BKM120以ATP竞争的方式特异性抑制PI3K / AKT激酶(或蛋白激酶B)信号传导途径中的I类PIK3,从而抑制次级信使磷脂酰肌醇-3,4,5-三磷酸的产生以及其活化。 PI3K信号通路。
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