gdc-0425

GDC-0425 (also known as RG-7602) is an orally available, highly selective small molecule inhibitor of checkpoint kinase 1 (Chk1). Chk1 is a serine/threonine-protein kinase that plays a critical role in the DNA damage response and cell cycle control. By inhibiting Chk1, GDC-0425 disrupts the cell’s ability to arrest the cell cycle and repair DNA damage, thereby enhancing the cytotoxic effects of DNA-damaging chemotherapies such as gemcitabine. The drug was developed by Genentech for use in various malignancies, particularly solid tumors and lymphoma. Clinical studies have shown that GDC-0425 can potentiate chemotherapy-induced tumor cell death but also cause manageable bone marrow suppression when combined with gemcitabine[1][2][4][8].

Other names

5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile