A80.2HCl

A80.2HCl is a novel orally available small molecule described as a "molecular glue" degrader of the MYC oncoprotein, developed by Kintor Pharmaceutical Ltd for oncology indications[1][3][4]. It induces degradation of MYC at nanomolar concentrations, restores pRB1 protein levels in cancer cells with high MYC expression, and re-sensitizes these cells to CDK4/6 inhibitors[1][2][3]. Mechanistically, it targets and inhibits Cyclin-dependent kinase 4 (CDK4), Cyclin-dependent kinase 6 (CDK6), and c-Myc (MYC) proteins[1]. Preclinical studies show that combining A80.2HCl with CDK4/6 inhibitors results in marked tumor regression in vivo by overcoming MYC-driven resistance to CDK4/6 inhibition[2][3].