RGNCY-0067 (16ae BRD4/HDAC inhibitor)

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16ae is a potent dual BRD4/HDAC inhibitor.  16ae exhibits significant anti-proliferative activities in vitro against human acute myelogenous leukemia (AML) cell lines.  It also has an inhibitory effect on Myc expression, and induces Myc in a concentration-dependent manner in human AML cells.  BRD4 IC50 >5000nM, HDAC IC50 = 204+21nM.

Systematic Name: (E)-3-(4-((4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)-2,6-dimethylphenoxy)methyl)phenyl)-N-hydroxyacrylamide

SMILES: COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCC3=CC=C(/C=C/C(NO)=O)C=C3)C

(C)=C2)=N4)=O)C4=C1

Formula:  C28H27N3O6

Mol Wt:  501.54

PMID:  28765013