biib021

BIIB021 is an orally available, fully synthetic small-molecule inhibitor of heat shock protein 90 (HSP90). It binds to the ATP-binding pocket of HSP90, interfering with its chaperone function and leading to degradation of client proteins involved in tumor growth and survival. This results in cell cycle arrest and apoptosis in cancer cells. BIIB021 is a purine scaffold-based compound and was the first synthetic HSP90 inhibitor to enter clinical trials. It has been evaluated for use in advanced solid tumors, gastrointestinal stromal tumors (GIST), B-cell chronic lymphocytic leukemia, lymphoma, and other cancers refractory to standard treatments. Unlike ansamycin-derived HSP90 inhibitors such as geldanamycin, BIIB021 does not demonstrate substantial hepatotoxicity.

Other names

6-chloro-9-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-9H-purin-2-amine