化合物CCT-251921 T14901

Product Introduction
Bioactivity


英文名: CCT-251921

描述: CCT-251921是一种有口服活性的选择性CDK8抑制剂；IC50值为2.3 nM。

体外活性: CCT-251921 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. And 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.

体内活性: CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties. The inhibition of STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) on day 15.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 15 mg/mL (36.51 mM)


关键字: CCT251921 | Cyclin dependent kinase | Inhibitor | CCT-251921 | CDK | inhibit | CCT 251921

相关产品: CDK4/6/1 Inhibitor | HTH-01-091 | H1k | XY028-140 | PROTAC CDK9 degrader-6 | FIT-039 | LRRK2-IN-1 | Amsilarotene | HS-243 | XPW1

相关库: Anti-Breast Cancer Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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