产品描述:
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}