GSK547

• CAT Number: I019199
• CAS Number: 2226735-55-1
• Molecular Formula: C₂₀H₁₈F₂N₆O
• Molecular Weight: 396.39
• Purity: ≥95%
• Storage: Store at -20°C
• IUPAC Name: 6-[4-[(3S)-3-(3,5-difluorophenyl)-3,4-dihydropyrazole-2-carbonyl]piperidin-1-yl]pyrimidine-4-carbonitrile
• InChI: 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
• InChIKey: SJVGFKBLUYAEOK-SFHVURJKSA-N
• SMILES: C1CN(CCC1C(=O)N2C(CC=N2)C3=CC(=CC(=C3)F)F)C4=NC=NC(=C4)C#N

GSK’547（Cat No.:I019199） is a highly selective and potent inhibitor of receptor-interacting protein kinase 1 (RIP1 or RIPK1). It exhibits a significant increase in oral exposure, approximately 400-fold, compared to GSK’963 based on a mouse pharmacokinetic study. By targeting RIP1, GSK’547 holds the potential in modulating cell death pathways and inflammatory responses. The increased oral exposure to GSK’547 suggests improved bioavailability, which may enhance its therapeutic efficacy.

Reference

[1]. Wang W, et al. RIP1 Kinase Drives Macrophage-Mediated Adaptive Immune Tolerance in Pancreatic Cancer. Cancer Cell. 2018 Nov 12;34(5):757-774.e7.