BI-4464 is a potent and selective small-molecule inhibitor targeting the KRAS G12C mutant protein, a key driver in certain cancers. It is primarily used in oncology research, especially for tumors harboring the KRAS G12C mutation, such as non-small cell lung cancer (NSCLC) and colorectal cancer. By covalently binding to the mutated cysteine residue in the KRAS protein, BI-4464 locks it in an inactive state, thereby blocking downstream signaling pathways like MAPK that promote cell proliferation and survival. This inhibition leads to reduced tumor growth in preclinical models. BI-4464 has served as a tool compound in the development of more advanced KRAS inhibitors and has contributed to understanding resistance mechanisms and combination therapy strategies, such as pairing with SHP2 or MEK inhibitors to enhance antitumor efficacy. Its application remains mainly in early-stage drug discovery and translational research.