BIIB021 is a potent, selective, orally available HSP90 inhibitor with Ki of 1.7 nM for Hsp90α.
BIIB021 displays no significant activity against a broad panel of protein kinases, and Na+K+ ATPase.
BIIB021 induces the degradation of Hsp90 client proteins including HER-2, AKT, and Raf-1 and upregulates expression of Hsp70 and Hsp27 in tumor cells.
BIIB021 inhibits cell growth and induces cell death in cell lines from a variety of tumor types at nanomolar concentrations (IC50=60 nM in N87 cells).
BIIB021 exhibits antitumor effects in vivo.
