Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MSC2530818 是一种有效的、选择性的、可口服的 CDK8 抑制剂,IC50值为2.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 461 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,870 | 现货 | ||
25 mg | ¥ 3,970 | 现货 | ||
50 mg | ¥ 5,660 | 现货 | ||
100 mg | ¥ 7,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,280 | 现货 |
产品描述 | MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM). |
靶点活性 | CDK8:2.6 nM (cell free) |
体外活性 | MSC2530818 binds to CDK8 and CDK19 with a similar affinity (4 nM). Potent inhibition of phospho-STAT1SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1SER727 IC50=8±2 nM). MSC2530818 demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. For example, MSC2530818 inhibits the reporter-based luciferase readout in several cell lines bearing activating WNT-pathway mutations; LS174T (β-catenin mutant, IC50=32±7 nM), COLO205 (APC mutant, IC50=9±1 nM) and demonstrates inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50=52±30 nM). Furthermore, MSC2530818 is a low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes. |
体内活性 | Tumor-bearing mice treated with MSC2530818 shows a reduction in tumor growth with T/C ratios (based on final tumor weights) of 49% and 57%, respectively. MSC2530818 is generally well tolerated, with no effects on mouse body weight in the qd administration schedule and manageable body weight loss. The human clearance and volume of distribution at steady-state are estimated to be low (0.14 L/h/kg) and small (0.48 L/kg), respectively, resulting in a short predicted terminal half-life (2.4 h). Physiologically based pharmacokinetics simulations suggested that human oral bioavailability maybe ≥75% up to a dose level of 500 mg daily. |
动物实验 | MSC2530818 is assessed in an established SW620 human colorectal cancer xenograft model in female NCr athymic mice. Tumor-bearing mice are treated orally with MSC2530818 (50 mg/kg bid or 100 mg/kg qd) for 16 days. Tumor weights are measured and body weights are monitored [1]. |
分子量 | 340.81 |
分子式 | C18H17ClN4O |
CAS No. | 1883423-59-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (352.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9342 mL | 14.6709 mL | 29.3419 mL | 73.3547 mL |
5 mM | 0.5868 mL | 2.9342 mL | 5.8684 mL | 14.6709 mL | |
10 mM | 0.2934 mL | 1.4671 mL | 2.9342 mL | 7.3355 mL | |
20 mM | 0.1467 mL | 0.7335 mL | 1.4671 mL | 3.6677 mL | |
50 mM | 0.0587 mL | 0.2934 mL | 0.5868 mL | 1.4671 mL | |
100 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7335 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。
MSC2530818 1883423-59-3 Cell Cycle/Checkpoint CDK Cyclin dependent kinase MSC-2530818 Inhibitor MSC 2530818 inhibit inhibitor