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| | IACS-9571 trifluoroacetate salt Basic information |
| | IACS-9571 trifluoroacetate salt Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO: 2mg/mL, clear | | form | powder | | color | white to beige | | InChIKey | GAOCLDPTFLDJIP-UHFFFAOYSA-N | | SMILES | 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 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | IACS-9571 trifluoroacetate salt Usage And Synthesis |
| Uses | A bromodomain Inhibitor. This domain contains proteins that are involved in the epigenetic regulation of gene expression and have been implicated in human cancer. | | Biological Activity | 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.). |
| | IACS-9571 trifluoroacetate salt Preparation Products And Raw materials |
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