BO-264

BO-264 is a potent, small-molecule inhibitor of transforming acidic coiled-coil 3 (TACC3), a protein frequently upregulated in various cancers and critical for microtubule stability and centrosome integrity. By targeting TACC3, BO-264 induces spindle assembly checkpoint-dependent mitotic arrest, DNA damage, and apoptosis. It has demonstrated significant antiproliferative activity across the NCI-60 cell line panel, particularly in aggressive breast cancer subtypes (basal and HER2+) and malignancies harboring FGFR3-TACC3 fusions. In preclinical studies, oral administration of BO-264 significantly impaired tumor growth in breast and colon cancer mouse models without major toxicity.