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AT7867 98%

货号:A151784

AT7867是一种ATP竞争性抑制剂,靶向Akt1/2/3和p70S6K/PKA,IC50分别为32nM/17nM/47nM和85nM/20nM,几乎不对AGC激酶家族以外的激酶具有抑制作用。

AT7867 化学结构 CAS号:857531-00-1
AT7867 化学结构
CAS号:857531-00-1
AT7867 3D分子结构
CAS号:857531-00-1
AT7867 化学结构 CAS号:857531-00-1
AT7867 3D分子结构 CAS号:857531-00-1
规格 价格 库存 数量
50μL*10mM(DMSO) ¥99随货¥69 现货 - +
10mM*1mL(DMSO) ¥562 现货 - +
1mg ¥302 现货 - +
2mg ¥451 现货 - +
5mg ¥756 现货 - +
10mg ¥1008 现货 - +
50mg ¥2079 咨询
100mg ¥3492 咨询
1g ¥15428 咨询
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AT7867 纯度/质量文件 产品仅供科研

货号:A151784 标准纯度: 98%
批次查询: 批次纯度:

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Nature Communications, 2025, 16, 1871. Ambeed. [ A508148 ]
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产品名称 Akt Akt1 Akt2 Akt3 其他靶点 纯度
Honokiol MEK 98%
PF-04691502 ++++

P-Akt (S473), IC50: 3.8 nM

P-Akt (T308), IC50: 7.5 nM

98+%
PHT-427 +

Akt, Ki: 2.7 μM

99%+
Deguelin PI3K 99%+
TIC10 isomer ERK 98+%
Perifosine +

Akt, IC50: 4.7 μM

98%
Miltefosine PKC,PI3K 98%
Triciribine +

Akt, IC50: 130 nM

99%+
Uprosertib +

Akt1, IC50: 180 nM

+

Akt2, IC50: 328 nM

++

Akt3, IC50: 38 nM

99%+
Afuresertib ++++

Akt1, Ki: 0.08 nM

++++

Akt2, Ki: 2 nM

++++

Akt3, Ki: 2.6 nM

99%+
Miransertib ++++

Akt1, IC50: 5 nM

++++

Akt2, IC50: 4.5 nM

++

Akt3, IC50: 16 nM

98+%
GSK-690693 ++++

Akt1, IC50: 2 nM

+++

Akt2, IC50: 13 nM

+++

Akt3, IC50: 9 nM

99%+
AT7867 ++

Akt1, IC50: 32 nM

++

Akt2, IC50: 17 nM

++

Akt3, IC50: 47 nM

PKA 99%+
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

+

Akt2, IC50: 210 nM

+

Akt3, IC50: 2119 nM

98+%
MK-2206 2HCl +++

Akt1, IC50: 8 nM

+++

Akt2, IC50: 12 nM

+

Akt3, IC50: 65 nM

99%+
Ipatasertib ++++

Akt1, IC50: 5 nM

++

Akt2, IC50: 18 nM

+++

Akt3, IC50: 8 nM

99%+
AT13148 ++

Akt1, IC50: 38 nM

+

Akt2, IC50: 402 nM

++

Akt3, IC50: 50 nM

PKA 95%
Capivasertib ++++

Akt1, IC50: 3 nM

+++

Akt2, IC50: 8 nM

+++

Akt3, IC50: 8 nM

99%+
A-674563 HCl +++

Akt1, Ki: 11 nM

PKA 99%
CCT128930 +++

Akt2, IC50: 6 nM

PKA 95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

AT7867 生物活性

靶点
  • Akt3

    Akt3, IC50:47 nM

  • Akt1

    Akt1, IC50:32 nM

  • Akt2

    Akt2, IC50:17 nM

描述 The protein kinase B (AKT) is a serine/threonine kinase that plays a pivotal role in tumor cell growth, malignant transformation, and chemoresistance. AT7867 is a potent inhibitor of three isoforms of AKT (AKT1, AKT2, and AKT3), the downstream kinase p70S6K, and PKA with IC50 values of 32, 17, 47, 20, and 85nM, respectively. AT7867 potently binds to AK2 in a ATP-competitive manner with a Ki value of 18nM. AT7867 inhibited the proliferation of multiple human cancer cell lines, including MES-SA, MDA-MB-468, MCF-7, U87MG, PC-3, DU145, HCT116, and HT29, with IC50 values in the range of 0.9–12µM. It also exerts an equipotent inhibitory effect on GSK3β phosphorylation across multiple cancer cell lines with IC50 values ranging from 2–4μM. The treatment of U87MG human glioblastoma cells with AT7867 induces apoptosis and suppressed AKT signaling in a concentration- and time-dependent manner. The administration of AT7867 (90mg/kg p.o. or 20mg/kg i.p.) significantly inhibited the phosphorylation of GSK3β and S6RP in mice bearing MES-SA tumors at 2 and 6 h following treatment. Mice treated with AT7867 at 20mg/kg i.p. showed a T/C ratio (tumor volume in treated mice versus control mice) of 0.37 on day 12. The T/C ratio in the group administered with AT7867 at 90mg/kg p.o. was 0.38 on day 10. [2]
作用机制 AT7867 binds to the ATP site of AK2, forming electrostatic interactions with the ribose site, hydrogen-bonding interactions with the kinase hinge region, and hydrophobic contacts with a lipophilic pocket in the glycine-rich loop.[2]

AT7867 参考文献

[1]Grimshaw KM, Hunter LJ, et al. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10.

[2]Grimshaw KM, Hunter LJ, Yap TA, et al. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010;9(5):1100‐1110. doi:10.1158/1535-7163.MCT-09-0986

AT7867 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.80mL

2.96mL

1.48mL

29.60mL

5.92mL

2.96mL

AT7867 技术信息

CAS号857531-00-1
分子式C20H20ClN3
分子量 337.846
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解方案

DMSO: 50 mg/mL(148 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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