详情描述
BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively). BI-9564 is useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases.
Product information
CAS Number: 1883429-22-8
Molecular Weight: 353.41
Formula: C20H23N3O3
Chemical Name: 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
Smiles: CN(C)CC1=CC(OC)=C(C=C1OC)C1=CN(C)C(=O)C2=CN=CC=C21
InChiKey: BJFSUDWKXGMUKA-UHFFFAOYSA-N
InChi: InChI=1S/C20H23N3O3/c1-22(2)11-13-8-19(26-5)15(9-18(13)25-4)17-12-23(3)20(24)16-10-21-7-6-14(16)17/h6-10,12H,11H2,1-5H3
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
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.
References:
- 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.