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。
Properties
Iupac Name: | 5-[2,6-di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine |
Inchi Code | 1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23) |
Inchi Key | CWHUFRVAEUJCEF-UHFFFAOYSA-N |
安全信息