计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC 50 of 2.3 nM.
In Vitro
CCT-251921 has acceptable aqueous solubility and demonstrates minimal activity when tested in a panel of 55 receptors, ion channels, and enzymes at 1 μM and in a panel of 279 kinases; weak inhibition of CYPs is observed. CCT-251921 demonstrates potent inhibition of reporter-based readouts measuring basal WNT pathway activity in human cancer cell lines that have constitutively activated WNT pathway signaling: LS174T (β-catenin mutant), SW480 and Colo205 (APC mutant) or PA-1 human teratocarcinoma cells that are WNT ligand dependent. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties in order to facilitate further evaluation of CDK8/19 pharmacology and progression into preclinical efficacy and safety studies. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) at day 15. The inhibition of STAT1 SER727 phosphorylation is maintained for more than 6 h after the last dose . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:CDK8 2.3 nM (IC 50 ) CDK19 2.6 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
CCT-251921
生化机理
CCT-251921 是一种强效、选择性和口服生物活性 CDK8 抑制剂，其 IC 50 为 2.3 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1C2=C(C=C(C=C2)C3=CN=C(C(=C3N4CCC5(CCNC5=O)CC4)Cl)N)C=N1
PubChem CID
分子量
410.90
技术文档
高级数据
关联靶点（人）
CDK8
Tchem
细胞周期蛋白依赖性激酶 8(Cyclin-dependent kinase 8)
(2 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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