BI-3663

BI-3663 is a highly selective, cereblon-based proteolysis-targeting chimera (PROTAC) that targets focal adhesion kinase (FAK, also known as PTK2) for proteasomal degradation. Developed by Boehringer Ingelheim in collaboration with the University of Dundee, BI-3663 is composed of the FAK inhibitor BI-4464 linked to the E3 ubiquitin ligase cereblon (CRBN) ligand pomalidomide. It potently degrades PTK2 with a median DC50 of 30 nM across various cancer cell lines, including hepatocellular carcinoma (HCC) and lung adenocarcinoma. Despite achieving robust protein degradation, BI-3663 has shown limited antiproliferative effects in preclinical models, making it primarily a valuable chemical probe for studying the scaffolding functions of FAK in biological systems.

Other names

BI 3663BI3663BI-3663