873837-23-1

溶解度:DMSO

储存条件:at -20℃ 2 years

生物活性

BIIB021,formerly CNF2024,is a novel fully synthetic inhibitor of Hsp90. It binds competitively with geldanamycin in the ATP-binding pocket of Hsp90 (Ki=1.7nM). [1]In tumor cells, BIIB021 induced the degradation of Hsp90 client proteins (including HER-2, AKT, and Raf-1) and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. BIIB021 inhibits cell growth and death in variety cell lines (breast, colon, lung) at nanomolar concentrations (IC50: 60nM-250nM) [1] . Oral administration of BIIB021 led to the inhibition of tumor growth in several human tumor xenograft models. BIIB021 is currently in phase I and II clinical trials in hematopoietic malignancies and solid tumors. [1]

参考文献

[1] Lundgren K et al. Mol Cancer Ther. 2009 Apr;8(4):921-9