AT7867 dihydrochloride
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.
对AKT1、AKT2、AKT3及PKA的IC50值分别为32 nM、17 nM、47 nM及20 nM。
丝氨酸/苏氨酸激酶AKT在参与恶性转化和化疗耐药的信号转导中起着关键作用,它是癌症治疗发展有吸引力的治疗靶点。基于结构的药物设计和基于片段的新药物发现鉴定到AT7867是一种新型的和强效的AKT激酶及其下游激酶p70 S6激酶 (p70S6K)的抑制剂,也是蛋白激酶A的抑制剂。
体外:AT7867强效抑制AKT和p70S6K活性,通过对GSK3β和S6核糖体蛋白磷酸化的抑制作用,以及对一系列人类癌症细胞系的生长抑制作用进行测定。用多种方法检测到AT7867用药后诱导肿瘤细胞凋亡[1]。
体内:在植入PTEN缺陷的U87MG人类胶质母细胞瘤异种移植无胸腺小鼠模型中,AT7867(90 mg/kg p.o.或20 mg/kg i.p.)引起下游底物AKT和p70S6K磷酸化的抑制,且诱发细胞凋亡。这些AT7867剂量也导致PTEN缺陷异种移植模型中人类肿瘤生长的抑制。这些发现表明,AKT和p70S6K阻滞的新型策略可能具有治疗价值,并有助于进一步评价AT7867作为一种单药的抗癌策略[1]。
临床试验:目前还没有临床数据。
参考文献:
[1] Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. 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):1100-10.
Storage | Store at -20°C |
M.Wt | 410.77 |
Cas No. | 1431697-86-7 |
Formula | C20H22Cl3N3 |
Synonyms | AT-7867 dihydrochloride;AT 7867 dihydrochloride |
Solubility | Soluble in DMSO |
Chemical Name | 4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine;dihydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl.Cl.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。 |