Name: BI-9564
Price: 246.00 USD

- Overview
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    Background
    
    IC50: 75 nM and 3.4 μM for BRD9 and BRD7 bromodomains, respectivelyBI-9564 is a BRD9/7 specific inhibitor.BRD7 and BRD9 are two important members of the bromodomain family protein. Both BRD7 and BRD9 have been implicated in chromatin remodeling.In vitro: BI-9564 was identified as a BRD9/7 specific inhibitor via fragment-based screening and structure-guided design. BI-9564 was found to be bind to BRD9 with a higher affinity than to BRD7, and was negative on BET family proteins. In addition, BI-9564 demonstrated in vitro off-target selectivity to CECR2, but not in cells [1]. In vivo: In animal study, BomTac:NMRIFoxn1nu mice were given two oral doses daily and the concentration of BI-9564 in plasma was measured. Dose-dependent AUCs were obtained for BI-9564, achieving exposures that were higher compared to the EC50 level for EOL-1 cells. Moreover, when the oral treatment with BI-9564 at 180 mg/kg was initiated on day 5 and applied daily with an interruption at day 18 and 19, a significant reduction in tumour growth compared to controls was found on day 18 leading to a median tumour growth inhibition value of 52% [1]. Clinical trial: Up to now, BI-9564 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
    
    CAS Number
    
    1883429-22-8
    
    Molecular Formula
    
    C20H23N3O3
    
    Molecular Weight
    
    353.41
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥8.82 mg/mL in DMSO with ultrasonic,≥8.32 mg/mL in EtOH with ultrasonic,insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BI-9564

BI-9564

Background

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