GDC-0575 is a potent and selective inhibitor of checkpoint kinase 1 (CHK1), a key protein involved in the DNA damage response pathway. It is primarily investigated for its use in cancer therapy, particularly in combination with DNA-damaging agents such as chemotherapy or radiation. By inhibiting CHK1, GDC-0575 prevents cancer cells from repairing DNA damage, leading to increased cell death, especially in tumors with underlying defects in cell cycle control or DNA repair mechanisms. It has shown promising activity in preclinical models of various solid tumors and hematological malignancies, including ovarian, lung, and pancreatic cancers. Its ability to enhance the efficacy of cytotoxic therapies makes it a candidate for overcoming resistance to standard treatments. GDC-0575 has advanced into clinical trials to evaluate its safety and effectiveness in combination regimens, focusing on patients whose tumors may be particularly vulnerable to CHK1 inhibition due to specific genetic backgrounds.