Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 11,700 | 6-8周 | ||
50 mg | ¥ 15,300 | 6-8周 | ||
100 mg | ¥ 19,500 | 6-8周 |
产品描述 | CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9). |
靶点活性 | CDK19-CyclinA:0.99 nM, CDK8-CyclinC:0.46 nM, CDK9:270 nM |
体外活性 | CDK8/19-IN-1 (52h) also weakly inhibits CDK2, with 62% inhibition at 1 μM. CDK8/19-IN-1 (1 μM) shows >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, CDC7. CDK8/19-IN-1 shows Kds of 25, 46, 81, 86, 97, 160, and >3000 nM for CDK19, CDK8, DYRK1B, HASPIN, YSK4, HIPK1, and EPHA3, respectively. CDK8/19-IN-1 displays potent antitumor activity (GI50: 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells). |
体内活性 | In mice bearing RPMI8226 human hematopoietic and lymphoid cells, CDK8/19-IN-1 (1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth. |
分子量 | 430.5 |
分子式 | C19H18N4O4S2 |
CAS No. | 1818427-07-4 |
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。
CDK8/19-IN-1 1818427-07-4 Cell Cycle/Checkpoint CDK CDK8/19IN1 CDK-8/19-IN-1 CDK8/19 IN 1 Inhibitor inhibitor inhibit