6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺
中文名称 | 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺 |
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中文同义词 | 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺 |
英文名称 | AZD-26 |
英文同义词 | AZD-26;3-PyridinecarboxaMide, 6-[4-(1-aMinocyclobutyl)phenyl]-5-pheny;6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamide;AKT-IN-1;AZD-26 ≥95%;AZD-26;AZD 26;AZD26;6-(4-(1-aminocyclobutyl)phenyl)-5-phenylnicotinamide;AKT inhibitor 1 |
CAS号 | 1357158-81-6 |
分子式 | C22H21N3O |
分子量 | 343.42 |
EINECS号 | |
相关类别 | |
Mol文件 | 1357158-81-6.mol |
结构式 |
6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺 性质
沸点 | 496.4±45.0 °C(Predicted) |
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密度 | 1.210±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 二甲基亚砜:25 mg/mL(72.80 mM) |
酸度系数(pKa) | 14.75±0.50(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
IC50: 1.042 μM (AKT)
AKT-IN-1 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC 50 s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40.
The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-18296 | AKT-IN-1 | 1 mg | 1142元 | |
2024/04/30 | HY-18296 | 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺 AKT-IN-1 | 1357158-81-6 | 5mg | 2500元 |