Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 < 20 μM) or CDK9/Cyclin T1 (IC50 < 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).
产品描述 | CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1). |
靶点活性 | CDK12:0.641 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50) |
体外活性 | CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC 50 =0.626 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC 50 =0.535 nM) and CAL-120 cells (IC 50 =2.43 nM)[1]. CDK12-IN-4 has a inhibition IC 50 CDK12 high ATP to Degradation DC 50 CDK12 ratio of 581[1]. |
别名 | CDK12-IN-4 |
分子量 | 426.432 |
分子式 | C20H20F2N8O |
CAS No. | 2651196-69-7 |
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。
CDK12-IN-4 2651196-69-7 CDK-12-IN-4 CDK12IN4 CDK12 IN 4 Inhibitor inhibitor inhibit