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概述
AT7867是ATP竞争性Akt1/2/3和p70S6K/PKA抑制剂，IC50分别为32 nM/17 nM/47 nM和85 nM/20 nM，对AGC激酶家族以外的蛋白几乎无活性。A potent ATP-competitive inhibitor of Akt1, Akt2 and Akt3
Information
AT7867 is a potent ATP-competitive inhibitor ofAkt1/2/3andp70S6K/PKAwithIC50of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family.
In vitro
AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50 of 20 nM and 85 nM, respectively. AT7867 shows ATP-competitive activity to Akt2 with Ki of 18 nM. AT7867 exhibits antiproliferation in cell lines with PTEN or PIK3CA mutations and shows great potent to MES-SA, MDA-MB-468, MCF-7, HCT116 and HT29 with IC50 of 0.94 μM, 2.26 μM, 1.86 μM, 1.76 μM and 3.04 μM, respectively. AT7867 also suppresses the cell growth of U87MG, PC-3 and DU145 cells with IC50 of 8.22 μM, 10.37 μM and 11.86 μM, respectively. AT7867 suppresses Akt activity by inhibiting phosphorylation of GSK-3β in human tumor cells with IC50 of 2-4 μM. AT7867 also induces the phosphorylation of the following Akt direct substrates including proapoptotic transcription factors FKHR (FoxO1a), FKHRL1 (FoxO3a) and the downstream target S6RP in U87MG cells.
In vivo
AT7867 shows bioavailability of 44% in mice by p.o. route. AT7867 could increase the cleaved PARP in MES-SA xenografts at 20 mg/kg i.p. or 90 mg/kg p.o.. AT7867 significantly inhibits the tumor growth in MES-SA xenografts or U87MG xenografts with T/C of 0.37 and 0.51, respectively.
Cell Data
cell lines：
Concentrations：0-100 μM , dissolved to a 10 mM stock in DMSO
Incubation Time：
Powder Purity:≥95%
规格
英文别名
4-(4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine
规格或纯度
10mM in DMSO
英文名称
AT7867
生化机理
AT7867 是 Akt1/2/3 和 p70S6K/PKA 的强效 ATP 竞争性抑制剂，在无细胞实验中的 IC50 分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM；在 AGC 激酶家族之外几乎没有活性。
储存条件
-80℃储存
运输条件
特低温运输
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
关联CAS
分子量
337.86
Reaxy-Rn
11072816
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11072816&ln=
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (354.24 mM);
沸点
530.2 °C/760 mmHg
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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