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BAY 1125976
产品别名
1402608-02-9
BAY 1125976
BAY1125976
2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide
BAY-1125976
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C23H21N5O |
| Molecular weight | 383.45 |
| MDL number | MFCD30481340 |
| Biochem/physiol Actions【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 models in 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. |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
