计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 / Akt2 / Akt3 and p70S6K / PKA with IC 50 s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
In Vitro
The inhibition of AKT2 by AT7867 is shown to be ATP-competitive with a K i of 18nM. AT7867 also displays potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC 50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC 50 values range from 10-12 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Following oral administration at 20 mg/kg, the elimination of AT7867 from plasma appears to be similar to that observed after i.v. administration. Plasma levels of AT7867 remain above 0.5 μM for at least 6 hours following an oral dose of 20 mg/kg. Assuming linear pharmacokinetics following i.v. administration, the bioavailability by the oral route is calculated to be 44%. In vivo pharmacodynamic (PD) biomarker studies are therefore performed with this model. Following pharmacokinetic and tolerability studies, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) are administered to athymic mice bearing MES-SA tumors and the phosphorylation status of GSK3β and S6RP in tumors is monitored over time. Clear inhibition of phosphorylation of the two markers of pathway activity is seen at 2 and 6 hours following treatment with AT7867. By 24 hours, total levels of both GSK3β and S6RP are greatly reduced . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Akt2 17 nM (IC 50 ) p70S6K 85 nM (IC 50 ) Akt1 32 nM (IC 50 ) Akt3 47 nM (IC 50 ) PKA 20 nM (IC 50 )
规格
别名
AT7867 二盐酸盐
规格或纯度
10mM in DMSO
英文名称
AT7867 dihydrochloride
生化机理
AT7867 二盐酸盐是 Akt1 / Akt2 / Akt3 和 p70S6K / PKA 的强效 ATP 竞争性抑制剂，IC 50 s 分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl.Cl.Cl
PubChem CID
分子量
410.77
技术文档
高级数据
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