产品详情
简单介绍:
BI-7273,BRD9BromodomainInhibitor
详情介绍:
Product Information
Molecular Weight: | 353.42 |
Formula: | C20H23N3O3 |
Purity: | ≥98% |
CAS#: | 1883429-21-7 |
Solubility: | DMSO up to 100 mM; Water up to 100 mM |
Chemical Name: | 4-(4-((dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one |
Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
BI-7273 is a potent, selective and cell-permeable BRD9 inhibitor with IC50 ~19 nM (Alpha assay). It also inhibits BRD7 with IC50 ~117 nM (Alpha assay). It has high selectivity against the other bromodomain family members (48 bromodomains) and kinases. In EOL-1 cellular proliferation assay, BI-7273 has IC50 at 1400 nM. It has very good pharmacokinetic profiling. BI-7273 together with BI-9546, could be useful chemical tools to further explore BRD9 bromodomain biology in both in vitro and in vivo settings.
How to Use:
In vitro: BI-7273 was used at 1-10 µM in vitro and cellular assays.
In vivo: BI-7273 was orally dosed to mice at 180 mg/kg once per day.
Reference:
- 1. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. (2016) J Med Chem. 59(10):4462-75.
Products are for research use only. Not for human use.
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