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Product Indentification


Name:   BIIB021
Synonyms:   BIIB021
CAS Registry Number:   848695-25-0
Molecular Formula:   C14H15ClN6O
Molecular Weight:    318.76
Molecular Structure:    



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Biological Activity of BIIB021:

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]
References on BIIB021:
[1] Lundgren K et al. Mol Cancer Ther. 2009 Apr;8(4):921-9

[2] Yin X et al. Int J Cancer. 2010 Mar 1;126(5):1216-25







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