BI-9564

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM, IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. It does not bind to other bromodomain-containing BET family members (IC50s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 µM. BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day). See the Structural Genomics Consortium (SGC) website for more information.Formal Name: 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one. CAS Number: 1883429-22-8. Molecular Formula: C20H23N3O3. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 5 mg/ml, Ethanol: 2 mg/ml. lambdamax: 249, 309 nm. SMILES: CN(C)CC1=CC(OC)=C(C(C2=C3C=NC=C2)=CN(C)C3=O)C=C1OC. InChi Code: 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. InChi Key: BJFSUDWKXGMUKA-UHFFFAOYSA-N.