BI-7273
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.
Reference:
[1] Martin LJ et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem.2016 May 26;59(10):4462-75.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 353.41 |
| Cas No. | 1883429-21-7 |
| Formula | C20H23N3O3 |
| Solubility | ≥35.3 mg/mL in DMSO with gentle warming; ≥1.99 mg/mL in EtOH with ultrasonic; ≥8.74 mg/mL in H2O |
| Chemical Name | 4-(4-((dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one |
| SDF | Download SDF |
| Canonical SMILES | O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C(OC)=C2)C3=CC=NC=C13 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
