3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮
中文名称 | 3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮 |
---|---|
中文同义词 | 3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮;AKT1变构抑制剂(AKT1 AND AKT2-IN-1);化合物 T14152;化合物 AKT1 AND AKT2-IN-1 |
英文名称 | 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one |
英文同义词 | 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one;Akti_2008;Akt1 and Akt2-IN-1;3-phenyl-2-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-1,6-naphthyridin-5(6H)-one;Akt1Akt2-IN-17;Akt1/2 inhibitor 1;1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-;Akt-1 and Akt2-IN-1,Akt1 and Akt2IN1,Akt1 and Akt2 IN 1 |
CAS号 | 893422-47-4 |
分子式 | C33H29N7O |
分子量 | 539.63 |
EINECS号 | |
相关类别 | 细胞生物学试剂;对照品 |
Mol文件 | 893422-47-4.mol |
结构式 |
3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮 性质
密度 | 1.285±0.06 g/cm3(Predicted) |
---|---|
储存条件 | Store at -20°C |
溶解度 | 二甲基亚砜:≥35mg/mL(64.86mM) |
酸度系数(pKa) | 7.99±0.40(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
Akt1 3.5 nM (IC 50 ) |
Akt2 42 nM (IC 50 ) |
Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC 50 =1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC 50 =5610 nM) and is a substrate for human P-glycoprotein.
Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-50862 | Akt1/Akt2-IN-1 | 1 mg | 1590元 | |
2024/08/19 | HY-50862 | 3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮 Akt1 and Akt2-IN-1 | 893422-47-4 | 5mg | 2800元 |