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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1607837-31-9
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1718.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥960.0 |
| 规格： | 5 mg | 产品价格： | ￥1900.0 |
| 规格： | 10 mg | 产品价格： | ￥2850.0 |
| 规格： | 25 mg | 产品价格： | ￥5130.0 |
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CCT-251921
CAS No. : 1607837-31-9
MCE 国际站：CCT-251921
产品活性：CCT-251921是有效，选择性，有口服活性的CDK8抑制剂；IC50值为2.3 nM。
研究领域：Cell Cycle/DNA Damage
作用靶点：CDK
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.
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 STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose.
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