Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK8-IN-11是一种高效且选择性的CDK8抑制剂,其IC50为46 nM。该化合物能够抑制WNT/β-catenin信号通路,主要用于结肠癌研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 5,930 | 10-14周 | ||
50 mg | ¥ 7,870 | 10-14周 | ||
100 mg | ¥ 11,100 | 10-14周 |
产品描述 | CDK8-IN-11 is a potent and selective inhibitor of CDK8, demonstrating an IC50 of 46 nM, and effectively targets the WNT/β-catenin signaling pathway. This compound has potential applications in colon cancer research [1]. |
体外活性 | CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% [1]. CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells [1]. CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells [1]. CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells [1]. CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells [1]. CDK8-IN-11 (0-4 μM) reverses Sorafenib resistance of HCT-116 cells [1]. Cell Proliferation Assay [1] Cell Line: HCT-116, HHT-29, SW480, CT-26, GES-1 cells Concentration: 0.08, 0.4, 2, 10, and 50 μM Incubation Time: 48 h Result: Inhibited cell proliferation with IC 50 values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively. Western Blot Analysis [1] Cell Line: HCT-116 cell Concentration: 0, 1, 2, 4 μM Incubation Time: 48 h Result: Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701. Cell Cycle Analysis [1] Cell Line: HCT-116 cell Concentration: 0.5-2 μM Incubation Time: 48 h Result: Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells. |
体内活性 | CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice [1]. CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days [1]. CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10 6 cm/s [1]. Animal Model: CT-26 xenograft mice [1] Dosage: 10 and 40 mg/kg Administration: Oral adminstration (p.o.) Result: Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor. Animal Model: Rats (pharmacokinetic assay) [1] Dosage: 10 mg/kg (p.o.), 2 mg/kg (i.v.) Administration: Oral adminstration (p.o.) or intravenous injection (i.v.) Result: Pharmacokinetic profile of CDK8-IN-11 (compound 29). dose (mg/kg) T 1/2 (h) T max (h) C max (ng/mL) F (%) 10 (p.o.) 1.1 0.8 453 31.7 2 (i.v.) 0.5 318 |
分子量 | 388.34 |
分子式 | C19H15F3N4O2 |
CAS No. | 2839338-28-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
CDK8-IN-11 2839338-28-0 Inhibitor inhibitor inhibit