BI-7273, BRD9 Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60322-2S 2 mg solid $129
M60322-10S 10mg solid $522

Description

Product Information
Molecular Weight: 353.41
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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