TY-1781

TY-1781 is a potent, highly selective small molecule inhibitor of cyclin-dependent kinase 2 (CDK2) developed by TYK Medicines. It exhibits excellent kinase inhibitory activity with an IC50 of 0.7 nM and demonstrates high selectivity over other CDK family members, including CDK1, CDK4, CDK6, CDK7, and CDK9. TY-1781 is designed to target tumors with CCNE1 (Cyclin E1) high expression or amplification, which is a key mechanism of resistance to CDK4/6 inhibitors. In preclinical models, TY-1781 has demonstrated robust anti-tumor activity as a monotherapy and in combination with CDK4/6 inhibitors, chemotherapy (such as gemcitabine), or PARP inhibitors, particularly in ovarian and breast cancer models.