AZD0156
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.
AZD0156是一种ATM激酶抑制剂。
共济失调毛细血管扩张症突变(ATM),来自磷脂酰肌醇3-激酶相关激酶(PIKK)蛋白激酶家族的一种丝氨酸/苏氨酸蛋白激酶,在DNA双链断裂激活的细胞DNA损伤应答信号传导中具有关键作用。活化的ATM可以促进DNA修复和S/G1细胞周期检查点,以防止早熟有丝分裂,维持基因组完整性以及促进适当的细胞存活或死亡途径。因此,ATM抑制剂可以代表肿瘤对化学/放射疗法高敏感性的有希望的临床机会。
体外:AZD0156被确定为首创可口服ATM抑制剂,在基于细胞的ATM抑制测定中显示出亚纳摩尔效力。此外,AZD0156具有比对PIKK家族酶其他成员高1000倍的选择性[1]。
体内:在动物研究中,AZD0156显示出优异的包括口服生物利用度在内的临床前PK性质。此外,在小鼠异种移植模型中,当与双链断裂(DSB)诱导剂组合时,AZD0156口服给药后显示出强效用[1]。
临床试验:AZD0156目前正在进行早期临床评估,以研究增加剂量的单独用药或与其他抗癌治疗联合用于晚期癌症患者的安全性和初步效果[2]。
参考文献:
[1] Kurt G. Pike. Identifying high quality, potent and selective inhibitors of ATM kinase: Discovery of AZD0156. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 4859.
[2] https://clinicaltrials. gov/ct2/show/NCT02588105term=AZD0156&rank=1
- 1. Needham, Jason M. "Manipulation and Dependence on Host Cell Cycle by Human RNA and DNA Viruses: Human Coronavirus OC43 and BK Polyomavirus." The University of Alabama at Birmingham ProQuest Dissertations & Theses, 2023. 30569807.
- 2. Chi-Wei Chen, Raquel Buj, et al. "ATM Inhibition Synergizes with Fenofibrate in High Grade Serous Ovarian Cancer Cells." Heliyon. 2020 Sep 29;6(9):e05097. PMID: 33024871
- 3. Kostaras E, Kaserer T, et al. "A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity." Br J Cancer. 2020;10.1038/s41416-020-0889-4. PMID: 32439931
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 461.56 |
Cas No. | 1821428-35-6 |
Formula | C26H31N5O3 |
Solubility | ≥23.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥5.49 mg/mL in EtOH |
Chemical Name | 8-(6-(3-(dimethylamino)propoxy)pyridin-3-yl)-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one |
SDF | Download SDF |
Canonical SMILES | O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3 |
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。 |
质量控制和MSDS
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