RGNCY-0107 (PDZ1i MDA-9/Syntenin PDZ1 inhibitor)

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PDZ1i is a targeted inhibitor of MDA-9/Syntenin PDZ1 domain which is a potential molecular target for prostate cancer.  By interacting with IGF-1, MDA-9/Syntenin activates STAT3 and regulates prostate cancer pathogenesis.  PDZ1i is well tolerated in vivo with a significant half life of 9h.  PDZ1i blocks prostate cancer cell in and migration in vitro and metastasis in vivo in immunocompetent mice.  Therefore, PDZ1i demonstrates potential as a therapy for prostate cancer, and possibly other cancers that express elevated MDA-9/Syntenin levels.

Systematic Name:  N-(2,5-dimethyl-4-(3-(5-phenyl-1,3,4-oxadiazol-2-yl)propanamido)phenyl)-8-oxo-5,6,7,8-tetrahydro-4H-cyclopenta[d][1,2,4]triazolo[1,5-a]pyrimidine-2-carboxamide

SMILES: O=C1C2=C(CCC2)NC3=NC(C(NC4=CC(C)=C(NC(CCC5=NN=C(C6=CC=

CC=C6)O5)=O)C=C4C)=O)=NN13

Formula:  C28H26N8O4

Mol Wt:   538.57

PMID:  31445950