THZ2 is a potent and selective CDK7 inhibitor with an IC 50 of 13.9 nM.
性状
Solid
IC50 & Target[1][2]
CDK7 13.9 nM (IC50) CDK1 96.9 nM (IC5
体外研究(In Vitro)
THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR breast cancer cells or normal human cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
THZ2 (10 mg/Kg) markedly reduces the growth rate of tumors in mice and demonstrates an anti-tumor activity. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis, as indicated by immunostaining against Ki67 and cleaved Caspase 3 respectively. THZ2 in NOD-SCID mice leads to reduced body weight, suggesting that THZ2 mayt be less well-tolerated in this particular mouse strain. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wang Y, et al. CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer. Cell. 2015 Sep 24;163(1):174-186.
溶解度数据
In Vitro: DMSO : 21.67 mg/mL (38.28 mM; Need ultrasonic)配制储备液