Please store the product under the recommended conditions in the Certificate of Analysis.
详情描述
CDK12-IN-5 是一种吡唑并三嗪,是有效的 CDK12 抑制剂,在高 ATP (2 mM) 下的 IC50 为 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。
产品详情
CDK12-IN-5 是一种吡唑并三嗪,是有效的 CDK12 抑制剂,在高 ATP (2 mM) 下的 IC50 为 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。
生物活性
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC 50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC 50 =173 μM) and CDK9/Cyclin T1 (IC 50 =127 μM) at high ATP (2 mM) (WO2021116178A1).
IC50 & Target[1][2]
CDK12 23.9 nM (IC50) CDK2/cyclinE 173 μM (
体外研究(In Vitro)
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM). CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.