RGNCY-0115 (Mortaparib mortalin/PARP1 inhibitor)

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Mortaparib is a novel compound that is a dual inhibitor of mortalin and PARP1 and demonstrates strong toxicity to ovarian, breast and cervical cancer cells.  Although Mortaparib can interact with mortalin, its binding with p53 is not stable.  However, it causes transcriptional repression of mortalin leading to p53 activation and growth arrest and apoptosis of cancer cells.  Mortaparib targets mortalin, PARP1 and mortalin/PARP1 interactions leading to inactivation of PARP1 which triggers growth arrest and apoptosis signalling.  Moertaparib treated cancer cells demonstrate inhibition of cell migration, metastasis and angiogenesis.  Mortaparib has also been shown to be a potent tumor suppressor in in vivo models and is a candidate for clinical development.

Systematic Name: 5-(1-(4-methoxyphenyl)-1H-tetrazol-5-yl)-4-phenylpyrimidin-2-amine

SMILES:  NC1=NC=C(C2=NN=NN2C3=CC=C(OC)C=C3)C(C4=CC=CC=C4)=N1

Formula:  C18H15N7O

Mol Wt:  345.37

PMID: 31856867