PDZ1i MDA-9/Syntenin PDZ1 inhibitor RGNCY-0107
Per 10 mg
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
Mol Wt: 538.57
Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin, Kegelman TP, etal. Proc. Natl. Acad. Sci. USA. 2017;114:370-375.
Suppression of prostate cancer pathogenesis using an MDA-9/Syntenin (SDCBP) PDZ1 small molecule inhibitor. Das, SK et al. Mol Cancer Ther. 2019 Jul 25. pii: molcanther.1019.2018. doi: 10.1158/1535-7163.MCT-18-1019. [Epub ahead of print].
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