| Identification | Back Directory | [Name]
BI-7273 | [CAS]
1883429-21-7 | [Synonyms]
BI273
CS-2327
BI-7273
BI 7273;BI7273
2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl- | [Molecular Formula]
C20H23N3O3 | [MDL Number]
MFCD30489736 | [MOL File]
1883429-21-7.mol | [Molecular Weight]
353.41 |
| Chemical Properties | Back Directory | [Boiling point ]
509.2±50.0 °C(Predicted) | [density ]
1.189±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥35.3 mg/mL in DMSO with gentle warming; ≥1.99 mg/mL in EtOH with ultrasonic; ≥8.74 mg/mL in H2O | [form ]
solid | [pka]
8.32±0.28(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM). It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 μM). | [Uses]
BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. | [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]. | [IC 50]
19 and 117 nm for brd9 and brd7, respectively. | [References]
[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. |
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