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IACS-9571 trifluoroacetate salt
产品别名
1883598-69-3
IACS-9571 trifluoroacetate salt
IACS 009571-001-4 trifluoroacetate
N-[6-[3-[4-(Dimethylamino)butoxy]-5-propoxyphenoxy]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide trifluoroacetate
N-(6-(3-(4-(Dimethylamino)butoxy)-5-propoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-3,4-dimethoxybenzenesulfonamide trifluoroacetate
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C32H42N4O8S · CF3CO2H |
| Molecular weight | 756.79 |
| Biochem/physiol Actions【生化/生理作用】 | IACS-9571 is a dimethylamine analogue. IACS-9571 is a high-affinity, potent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nM, BAZ2B/TAF1 BrD2/BRD4 BrD1,2 Kd = 0.4/1.8/>10 μM by DiscoveRx; ≤63% binding inhibition of 25 other BrDs at 1 μM). IACS-9571 potently blocks H3K23Ac peptide from TRIM24 BrD binding (IC50 = 7.6 nM) and displaces ectopically expressed TRIM24 PHD-BrD from endogenous histone H3 in 2-hr 5 μM SAHA-stimulated HeLa cells (IC50 = 50 nM). When adiministered in mice, IACS-9571 exhibits good pharmacokinetics and oral availability in vivo (F = 29%, 10 mg/kg p.o.). |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=S(C1=CC=C(C(OC)=C1)OC)(NC2=C(C=C(C3=C2)N(C(N3C)=O)C)OC4=CC(OCCC)=CC(OCCCCN(C)C)=C4)=O.FC(F)(C(O)=O)F |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
