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).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
