|
|
| | BI-7273 Basic information |
| Product Name: | BI-7273 | | Synonyms: | BI-7273;BI273;2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-;CS-2327;BI 7273;BI7273;inhibit,Inhibitor,Epigenetic Reader Domain,BI7273,BI-7273,BI 7273;4-(4-((dimethylamino)methyl)-2,6-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one | | CAS: | 1883429-21-7 | | MF: | C20H23N3O3 | | MW: | 353.41 | | EINECS: | | | Product Categories: | | | Mol File: | 1883429-21-7.mol |  |
| | BI-7273 Chemical Properties |
| 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 |
| | BI-7273 Usage And Synthesis |
| 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). | | 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. |
| | BI-7273 Preparation Products And Raw materials |
|