CC-115
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.
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
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