半岛bd体育手机客户端 说明
生化/生理作用
BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC50= 5.2/18 nM with 10 μM ATP, IC50= 44/36 nM with 2 mM ATP; AKT3 IC50= 427 nM with 10 μM ATP) that targets a pocket formed by the kinase & PH domain. BAY 1125976 reduces basal AKT T308/S473 phosphorylation (IC50= 0.9/1.1; KPL-4 cells) and exhibits anti-cancer efficacy in cultures (IC50= 0.02-10 μM, 23 human cancer lines) and in xenograft modelsin vivo(25, 50 mg/kg/day or 5, 15, 25 mg/kg bid. po.; mice), including breast cancers (KPL4 PIK3CAH1074R mutant, MCF7, HBCx-2), AKTE17K-driven prostate cancer LAPC-4, and anal cancer AXF 984.
基本信息
| 经验(实验)分子式 | C23H21N5O |
| 分子量 | 383.45 |
| MDL编号 | MFCD30481340 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
