应用 |
A potent inhibitor the PI 3-kinase family |
产品介绍 |
GDC-0941是PI3Kα/δ抑制剂,IC50为3 nM,比对p110β和p110γ的抑制性强11倍和25倍。 |
备注 |
GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).Phase 2 |
生化机理 |
GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. GDC-0941 against p110a IC50=0.003μM,U87MG IC50=0.95μM, A2780 IC50=0.14 μM, and in vitro metabolic stability in mouse and human is 91.96%. The inhibitions of U87MG , PC3, MDA-MB-361 cancer cell proliferation are (IC50) 0.95, 0.28, 0.72 μM, respectively. |
别名 |
GDC 0941;GDC0941; 2-(1H-吲唑-4-基)-6-((4-(甲基磺酰基)-1-哌嗪基)甲基)-4-(4-吗啉基)噻吩并(3,2-d)嘧啶;;Pictrelisib;GDC 0941;GDC0941; 2-(1H-Indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine |