BI-7273
- Product Name
- BI-7273
- CAS No.
- 1883429-21-7
- Chemical Name
- BI-7273
- Synonyms
- BI273;BI-7273;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;2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-
- CBNumber
- CB53128809
- Molecular Formula
- C20H23N3O3
- Formula Weight
- 353.41
- MOL File
- 1883429-21-7.mol
BI-7273 Property
- 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
N-Bromosuccinimide Price
- Product number
- 20311
- Product name
- BI-7273
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 20311
- Product name
- BI-7273
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 20311
- Product name
- BI-7273
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 20311
- Product name
- BI-7273
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $573
- Updated
- 2024/03/01
- Product number
- B6196
- Product name
- BI-7273
- Packaging
- 5mg
- Price
- $103
- Updated
- 2021/12/16
BI-7273 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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