AT7867
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AT 7867是Akt1/2/3和p70S6K/PKA的有效的ATP竞争性抑制剂,对Akt1、Akt2、Akt3 、p70S6K和PKA的IC50分别为32 nM、17 nM、47 nM 、85 nM和20 nM。
Akt也被称为蛋白激酶B,是一种丝氨酸/苏氨酸特异性蛋白激酶,在多种细胞过程中起关键作用,例如葡萄糖代谢、细胞凋亡、细胞增殖、转录和细胞迁移。
AT7867抑制多种人类肿瘤细胞系的细胞增殖,例如MES-SA子宫癌、MDA-MB-468 、MCF-7乳腺癌、HCT116 、HT29结肠癌,IC50为0.9-3 μM。AT7867同时抑制这些细胞系的GSK3β,IC50为2-4 μM之间。在U87MG人胶质母细胞瘤细胞中,AT7867抑制AKT信号,以浓度和时间依赖性方式诱导细胞凋亡[1]。
在PTEN缺失的U87MG人胶质母细胞瘤异种移植裸鼠模型中,AT7867抑制AKT / p70S6K下游底物的磷酸化,导致细胞凋亡。在PTEN缺失异种移植模型中,AT7867抑制人体肿瘤的生长[1]。
参考文献:
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 May;9(5):1100-10.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 337.85 |
Cas No. | 857531-00-1 |
Formula | C20H20ClN3 |
Solubility | ≥16.9 mg/mL in DMSO; ≥4.38 mg/mL in EtOH with ultrasonic; ≥45 mg/mL in H2O |
Chemical Name | 4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine |
SDF | Download SDF |
Canonical SMILES | C1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | AT 7867是Akt1/2/3和p70S6K/PKA的有效ATP竞争性抑制剂,对Akt1、Akt2、Akt3 、p70S6K和PKA的IC50分别为32 nM、17 nM、47 nM 、85 nM和20 nM。 | |||||
靶点 | Akt2 | PKA | Akt1 | Akt3 | p70 S6K | |
IC50 | 17 nM | 20 nM | 32 nM | 47 nM | 85 nM |
质量控制和MSDS
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