BO-264 (BO264) is a highly potent inhibitor of transforming acidic coiled-coil (TACC) family member TACC3 (IC50=188 nM).
The interaction between TACC3 and BO-264 with a dissociation constant, KD of 1.5 nM.
BO-264 inhibits the viability of cancer cells with FGFR3–TACC3 fusion and shows very potent cytotoxicity in NCI-60 cancer cell line panel.
TACC3 inhibition with BO-264 induces mitotic arrest, apoptosis, and DNA damage, causes aberrant spindle formation, and reduces centrosomal localization of TACC3.
BO-264 significantly impairs tumor growth and improves survival in in vivo xenograft and syngeneic models without major toxicity.
