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CAS No.: 857531-00-1

AT7867 Catalog No. CSN16097

Synonyms: At7867

AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, exhibiting little activity outside the AGC kinase family.

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生物活性

实验方案

技术信息

生物活性

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 K_i 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]
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9599 mL
- 14.7996 mL
- 29.5993 mL
- 5 mM
- 0.5920 mL
- 2.9599 mL
- 5.9199 mL
- 10 mM
- 0.2960 mL
- 1.4800 mL
- 2.9599 mL

技术信息

CAS号

857531-00-1

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H20ClN3

运输

蓝冰

分子量

337.85

别名

At7867

溶解度

DMSO	68.0 mg/mL (201.3 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (14.8 mM)

动物实验配方

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