BMS-599626/BMS599626

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BMS-599626/BMS599626

BMS-599626/BMS599626

Cat.No.ABP000838 Chemical NameBMS-599626/BMS599626 CAS873837-23-1 MolFormulaC27H28ClFN8O3 MolWeight567.014 Purity 99%

Chemical Name : BMS-599626/BMS599626

CAS : 873837-23-1

Synonyms: [4-[[1-[(3-Fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid (3S)-3-morpholinylmethyl ester hydrochloride

Solubility:DMSO

Storage:at -20℃ 2 years

Biologieal

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]

Reference

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

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