|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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.
- Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. (2016) J Med Chem. 59(10):4462-75.
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