RGNCY-0109 (GSK3145095 RIP1 Kinase inhibitor)

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GSK3145095 is an inhibitor of RIP1 which regulates cell death and inflammation playing an important role contributing to a variety of human pathologies including immune-mediated inflammatory disease and cancer.  GSK3145095 binds specifically and potently to RIP1 and significantly blocks RIP1 kinase-dependent cellular responses.  GSK3145095 also promotes tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures further demonstrating its potential as a novel cancer therapy. GSK3145095 is currently in Phase 1 clinical trial for pancreatic adenocarcinoma and a number of other sold tumors. 

Systematic Name: (S)-5-benzyl-N-(7,8-difluoro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-1H-1,2,4-triazole-3-carboxamide

SMILES:  FC1=CC2=C(NC([C@@H](NC(C3=NNC(CC4=CC=CC=C4)=N3)=O)CC2)=O)C=C1F

Formula:   C20H17F2N5O2

Mol Wt:   397.39

PMID:  31223438