| Molecular Weight: | 353.42 |
| Formula: | C20H23N3O3 |
| Purity: | ≥98% |
| CAS#: | 1883429-22-8 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
BI-9546 is a potent, selective and cell-permeable BRD9 inhibitor with IC50 ~75 nM (Alpha assay). It has good selectivity over BRD7 (IC50 ~3410 nM, Alpha assay). It has high selectivity against the other bromodomain family members (48 bromodomains) and kinases. In EOL-1 cellular proliferation assay, BI-9546 has IC50 at 800 nM. It has very good pharmacokinetic profiling, and also displays antitumor activity in EOL-1 AML xenograft model with oral treatment. BI-9546 could be a useful chemical tool to further explore BRD9 bromodomain biology in both in vitro and in vivo settings.
How to Use:
In vitro: BI-9546 was used at 1-10 µM in vitro and cellular assays.
In vivo: BI-9546 was orally dosed to mice in EOL-1 AML xenograft model 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.
