Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT-251921是一种有口服活性的选择性CDK8抑制剂;IC50值为2.3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 795 | 现货 | ||
2 mg | ¥ 1,060 | 现货 | ||
5 mg | ¥ 1,570 | 现货 | ||
10 mg | ¥ 2,360 | 现货 | ||
25 mg | ¥ 4,250 | 现货 | ||
50 mg | ¥ 5,950 | 现货 | ||
100 mg | ¥ 7,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,730 | 现货 |
产品描述 | CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM). |
靶点活性 | CDK19:2.6 nM (IC50), CDK8:2.3 nM (IC50) |
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. |
分子量 | 410.9 |
分子式 | C21H23ClN6O |
CAS No. | 1607837-31-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15 mg/mL (36.51 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4337 mL | 12.1684 mL | 24.3368 mL | 60.8421 mL |
5 mM | 0.4867 mL | 2.4337 mL | 4.8674 mL | 12.1684 mL | |
10 mM | 0.2434 mL | 1.2168 mL | 2.4337 mL | 6.0842 mL | |
20 mM | 0.1217 mL | 0.6084 mL | 1.2168 mL | 3.0421 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CCT-251921 1607837-31-9 Cell Cycle/Checkpoint CDK CCT251921 Cyclin dependent kinase Inhibitor inhibit CCT 251921 inhibitor