Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
General description
BIIB021 is a purine scaffold-based second-generation heat shock protein 90 (Hsp90) inhibitor.
Application
BIIB021 may be used to study its effect on growth of natural killer (NK) cells and T cell lymphomas.
Biochem/physiol Actions
BIIB021 (CNF2024) is an orally active, potent and selective heat shock protein 90 (Hsp90) inhibitor that targets the ATP site of Hsp90 (Ki = 1.7 nM against 2 nM FITC-geldanamycin in competitive binding for 0.8 nM rhHsp90α), but not those of 20 cellular kinases or Na+/K+ ATPase. BIIB021 induces Her-2 degradation in MCF7 cells (IC50 = 38 nM post 16h incubation) and exhibits anti-cancer efficacy in cultures (IC50 = 60-310 nM among 8 cancer lines) and in mice in vivo (51-94% tumor growth inhibition among 6 human tumor models; 75-125 mg/kg/d 5x per wk for 5 wks).
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Srinivas R Kasibhatla et al.
Journal of medicinal chemistry, 50(12), 2767-2778 (2007-05-10)
Heat shock protein 90 (Hsp90) is a molecular chaperone protein implicated in stabilizing the conformation and maintaining the function of many cell-signaling proteins. Many oncogenic proteins are more dependent on Hsp90 in maintaining their conformation, stability, and maturation than their
Karen Lundgren et al.
Molecular cancer therapeutics, 8(4), 921-929 (2009-04-18)
Inhibition of heat shock protein 90 (Hsp90) results in the degradation of oncoproteins that drive malignant progression, inducing cell death, making Hsp90 a target of substantial interest for cancer therapy. BIIB021 is a novel, fully synthetic inhibitor of Hsp90 that
Boris Böll et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 15(16), 5108-5116 (2009-08-13)
In Hodgkin's lymphoma, constitutive activation of NF-kappaB promotes tumor cell survival and proliferation. The molecular chaperone heat shock protein 90 (HSP90) has immune regulatory activity and supports the activation of NF-kappaB in Hodgkin's lymphoma cells. We analyzed the effect of
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