Name: BI-7273
Price: 265.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 19 and 117 nM for BRD9 and BRD7, respectively.BI-7273 is a BRD9 bromodomain inhibitor.BRD9, a SWI/SNF subunit, is identified to have a key role in leukemia growth, and the BRD9 bromodomain (BD) has been shown to be critical for the proliferation of acute myeloid leukemia cells.In vitro: BI-7273 was previously demonstrated to mimic genetic perturbation of BRD9. BI-7273 could also target BRD7 BD, a BD protein that was found in a subclass of SWI/SNF remodelling complexes sharing high sequence homology with BRD9. In addition, BI-7273 was able to form an additional positive interaction with the carbonyl of Asn100 in BRD9. Furthermore, BI-7273 showed no measurable activity against BET family BDs even up to a concentration of 100 μM in the biochemical Alpha assay [1]. In vivo: In order to explore the potential of BI-7273 as in-vivo chemical probe, female BomTac:NMRIFoxn1nu mice was orally administered two doses at 20 and 180 mg/ kg and the concentration of BI-7273 in plasma over time was measured. Results showed that dose-dependent but nonlinear AUC was observed for BI-7273, achieving exposure that was higher compared to the EC50 level determined for BI-7273 in proliferation assays with EOL-1 cells [1]. Clinical trial: Up to now, BI-7273 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    4-(4-((dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
    
    CAS Number
    
    1883429-21-7
    
    Molecular Formula
    
    C20H23N3O3
    
    Molecular Weight
    
    353.41
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥35.3 mg/mL in DMSO with gentle warming; ≥1.99 mg/mL in EtOH with ultrasonic; ≥8.74 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BI-7273

BI-7273

Background

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