CC-115
![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.
作用于mTOR/DNA-PK,IC50为21/13 nM。
CC-115是一种mTOR/DNA-PK抑制剂。
MTOR是磷酸肌醇3-激酶/蛋白激酶B(AKT途径)的一种关键介质。DNA依赖性蛋白激酶(DNA-PK)是DNA修复机制的关键组成部分,其控制对DNA损伤的应答,用于维持基因组完整性。
体外:先前研究发现,CD40(+)白细胞介素-21刺激诱导的增殖可以被CC-115完全阻断,并且CD40介导的对fludarabine和venetoclax的抗性也可以被CC-115逆转。此外,在来自对idelalisib具有获得性抗性的患者CLL样品中,BCR介导的信号传导被CC-115阻断[1]。
体内:临床前研究显示,CC-115在多个物种中具有良好的体内PK曲线,在小鼠、大鼠和犬类中分别具有53%、76%和约100%的口服生物利用度[2]。
临床试验:在携带ATM缺失/突变的8例复发/难治性CLL/小淋巴细胞淋巴瘤患者中研究CC-115的临床疗效。结果显示,除一名患者外,所有患者的淋巴结病减少,导致1例IWCLL部分反应(PR)和3例伴有淋巴细胞增多的PR。这些早期有希望的临床活性表明CC-115可进一步研究用于治疗CLL[1]。
参考文献:
[1] Thijssen R,et al. Dual TORK/DNA-PK inhibition blocks critical signaling pathways in chronic lymphocytic leukemia. Blood.2016 Jul 28;128(4):574-83.
[2] Mortensen DS, et al. Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. J Med Chem. 2015 Jul 23;58(14):5599-5608.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 336.35 |
Cas No. | 1228013-15-7 |
Formula | C16H16N8O |
Solubility | ≥50 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,5-dihydropyrazino[2,3-b]pyrazin-2(1H)-one |
SDF | Download SDF |
Canonical SMILES | CCN1C(CN=C2C1=NC(C(C=CC(C3=NNC=N3)=N4)=C4C)=CN2)=O |
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
- 批次:
化学结构
![CC-115](http://www.apexbt.com//media/diy/images/struct/B6114.png)