Formulation: A solid
Formal Name: 6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-4-pyrimidinecarbonitrile
Purity: ≥98%
Formula Markup: C20H18F2N6O
Formula Weight: 396,4
Shelf life (days): 1460
CAS Number: 2226735-55-1
Notes: GSK547 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1; IC50 = 31 nM).{72066} 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-α and IL-1β and decreases macrophage infiltration in aortic sinus lesions in an ApoESA/SA mouse model of early-phase atherogenesis.{72067}
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