Nu 6027
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NU6027是一种有效的细胞ATR活性抑制剂,IC50值为6.7 μM。
共济失调毛细血管扩张突变和Rad3相关激酶(ATR)在复制叉停滞信号和DNA损伤到细胞周期检验点和DNA修复中具有关键作用。ATR被认为是癌症治疗的关键靶点,但是,其抑制剂难以实现。NU6027这一最早作为CDK2抑制剂开发的产品,可抑制ATR。
体外实验:NU6027是一种有效的细胞ATR活性抑制剂,IC50值为6.7 μM,并能够通过ATR依赖的方式增加羟基脲和顺铂的细胞毒性。NU6027可衰减G2/M期停滞,并伴随DNA损伤,抑制RAD51病灶的形成,并能增加主要类别的DNA损坏细胞毒药物疗法(非紫杉醇和抗有丝分裂药)的细胞毒性。在A2780细胞中,具有功能性p53和错配修复的细胞对顺铂的敏感性最大,而具有功能性错配修复功能的p53突变细胞对替莫唑胺的敏感性最大。更重要的是,当聚(ADP-核糖)聚合酶(PARP)抑制或XRCC1缺陷引起DNA单链断裂修复受损时,NU6027具有综合致死功能[1]。
体内实验:目前无体内实验结果。
临床试验:NU6027仍处于临床前研究阶段,尚未进行临床试验。
参考文献:
[1] Peasland A, Wang LZ, Rowling E, Kyle S, Chen T, Hopkins A, Cliby WA, Sarkaria J, Beale G, Edmondson RJ, Curtin NJ. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011;105(3):372-81.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 251.28 |
Cas No. | 220036-08-8 |
Formula | C11H17N5O2 |
Solubility | insoluble in H2O; ≥12.55 mg/mL in DMSO; ≥2.72 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine |
SDF | Download SDF |
Canonical SMILES | C1CCC(CC1)COC2=NC(=NC(=C2N=O)N)N |
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 | Nu 6027是一种有选择性的CDK1和CDK2抑制剂,IC50值分别为2.9和2.2 ?M。 | |||||
靶点 | CDK1 | CDK2 | ||||
IC50 | 2.9 ?M | 2.2 ?M |
化学结构
![Nu 6027](http://www.apexbt.com//media/diy/images/struct/A1986.png)