GSK547

GSK547 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1, IC50 = 31 nM). It is selective for RIPK1 over a panel of 371 kinases, including RIPK2, -3, -4, and -5, at 10 µM. In vivo, GSK547 (100 mg/kg) increases survival and reduces tumor volume and the number of liver metastases in a P48Cre KrasG12D orthotopic mouse model of progressive pancreatic ductal adenocarcinoma (PDA). Adoptive transfer of tumor-infiltrating T cells isolated from GSK547-treated mice protects against orthotopic PDA tumor growth in mice. GSK547 also reduces plasma levels of TNF-alpha and IL-1beta and decreases macrophage infiltration in aortic sinus lesions in an ApoESA/SA mouse model of early-phase atherogenesis.Formal Name: 6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-4-pyrimidinecarbonitrile. CAS Number: 2226735-55-1. Synonyms: RIP1i. Molecular Formula: C20H18F2N6O. Formula Weight: 396.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: Slightly soluble, Ethanol: Slightly soluble. lambdamax: 256 nm. SMILES: N#CC1=CC(N2CCC(C(N3N=CC[C@@]3([H])C4=CC(F)=CC(F)=C4)=O)CC2)=NC=N1. InChi Code: InChI=1S/C20H18F2N6O/c21-15-7-14(8-16(22)9-15)18-1-4-26-28(18)20(29)13-2-5-27(6-3-13)19-10-17(11-23)24-12-25-19/h4,7-10,12-13,18H,1-3,5-6H2/t18-/m0/s1. InChi Key: SJVGFKBLUYAEOK-SFHVURJKSA-N.