THZ2

THZ2 is a potent and selective CDK7 inhibitor with an IC₅₀ of 13.9 nM. IC50 & Target: IC50: 13.9 nM (CDK7)^[1] 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^[1]. 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^[1].