store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50 = 173 μM) and CDK9/Cyclin T1 (IC50 = 127 μM) at the same high ATP concentration of 2 mM, as stated in WO2021116178A1.
产品描述 | CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50 = 173 μM) and CDK9/Cyclin T1 (IC50 = 127 μM) at the same high ATP concentration of 2 mM, as stated in WO2021116178A1. |
靶点活性 | CDK12:23.9 nM (IC50), CDK2-CyclinE:173 μM (IC50), CDK9-CyclinT1:127 μM (IC50) |
体外活性 | CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC 50 =3.23 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC 50 =4.19 nM) and CAL-120 cells (IC 50 =3.57 nM)[1]. CDK12-IN-5 has a inhibition IC 50 CDK12 high ATP to Degradation DC 50 CDK12 ratio of 32[1]. |
别名 | CDK12-IN-5 |
分子量 | 454.365 |
分子式 | C18H15F5N8O |
CAS No. | 2651200-35-8 |
store at low temperature | 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-5 2651200-35-8 CDK-12-IN-5 CDK12IN5 CDK12 IN 5 Inhibitor inhibitor inhibit