CCT244747
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.
IC50: 29-170 nM
CHK1是一种丝氨酸/苏氨酸激酶,可以被直接的DNA损伤或复制压力造成的DNA单链断裂(SSBs)激活. CHK1的激活启动细胞周期停滞的信号级联反应,最终导致DNA修复\衰老或死亡.通过一系列化疗剂抑制CHK1,废除DNA损伤后的细胞周期阻滞\抑制DNA修复并诱导肿瘤细胞死亡.CCT244747是CHK1的强效选择性抑制剂.
体外实验:在多种肿瘤细胞系中,CCT244747抑制细胞内CHK1活性,显著增强几种抗癌药物的细胞毒性,废除药物诱导的S和G2期阻滞.CHK1活性和细胞周期活动的生物标志物是由基因毒性诱导的,可以被CCT244747抑制,增强DNA损伤和细胞凋亡[1].
在体实验:口服给药CCT244747后得到其活性的肿瘤浓度.在人肿瘤异种移植模型中,CCT244747显著增强吉西他滨和伊立替康的抗肿瘤活性,表明CHK1抑制伴随生物标志物的调制[1].
临床试验:到目前为止,CCT244747还处于临床前开发阶段.
参考文献：
[1] Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clin Cancer Res. 2012 Oct 15;18(20):5650-61.
| Storage | Store at -20°C |
| M.Wt | 408.46 |
| Cas No. | 1404095-34-6 |
| Formula | C20H24N8O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | (R)-3-((1-(dimethylamino)propan-2-yl)oxy)-5-((4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)pyrazine-2-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | C[C@](OC1=NC(NC(C=C2OC)=NC=C2C(C=N3)=CN3C)=CN=C1C#N)([H])CN(C)C |
| 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。 |
化学结构
