RGNCY-0122 (6Br-6a STAT3 inhibitor)

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6Br-6a is a novel STAT3 inhibitor.  Stat3 protein is overexpressed in many malignancies  yet there is no STAT3 inhibitor used clinically.  6Br-6a was shown to induce cell cycle arrest and apoptosis (by regulating cyclin D1 and Bcl-2) in breast cancer cell lines MDA-MB-231 and MCF-7 in vitro and in vivo in xenograft mouse models with effective tumor inhibition.  6Br-6a may be a potential candidate for the treatment of breast cancer.

Systematic Name: (E)-1-(4-(4-bromo-1,1-dioxidocinnamoyl)piperazin-1-yl)-3-(3,4-dimethoxyphenyl)prop-2-en-1-one

SMILES:  BrC1=C2C(S(C(C(N3CCN(C(/C=C/C4=CC(OC)=C(OC)C=C4)=O)CC3)=O)=C2)(=O)=O)=CC=C1

Formula:   C24H23BrN2O6S

Mol Wt: 547.42