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BIIB021

Cat No.
CEI-0987
Description
BIIB021 is an orally available, synthetic small-molecule Hsp90 inhibitor. It binds in the ATP-binding pocket of Hsp90 (Ki = 1.7 ± 0.4 nM) and induces HER-2 degradation with an EC50 of 38 ± 10 nM in MCF-7 cells. It ncreases expression of the heat shock proteins Hsp90α and Hsp70, but has no effect on expression of the nonclient protein phosphatidylinositol 3-kinase p85 subunit. BIIB021 inhibits the proliferation of N87, MCF-7, and BT474 tumor cells with IC50 values of 0.06, 0.31, and 0.14 µM, respectively. It has significant antitumor activity in N87 stomach, BT474 breast, CWR22 prostate, U87 glioblastoma, SKOV3 ovarian, and Panc-1 pancreatic tumor xenograft models.
Abbr
BIIB021(HSP90AA1)
Alias
EL52, HSP86, HSP89A, HSP90A, HSP90N, HSPC1, HSPCA, HSPCAL1, HSPCAL4, HSPN, Hsp89, LAP2
Appearance
Off-white or light brown powder
CAS No.
848695-25-0
Molecular Weight
318.8 Da
Purity
>99%
Stability
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Synonyms
EL52, HSP86, HSP89A, HSP90A, HSP90N, HSPC1, HSPCA, HSPCAL1, HSPCAL4, HSPN, Hsp89, LAP2
Targets
HSP90
IC50
N87, MCF-7, and BT474 tumor cells:IC50 0.06, 0.31, and 0.14 µM, respectively
Molecular Formula
C14H15ClN6O
Solubility
Soluble in DMSO at 65 mg/ml; soluble in ethanol at 3 mg/ml with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM.
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