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CAS No. | 2226735-55-1 | Cat. No. | BCP30590 |
Name | GSK547 | ||
Synonyms | GSK-547; GSK 547; RIP1i; | ||
SMILES | C1CN(CCC1C(=O)N2C(CC=N2)C3=CC(=CC(=C3)F)F)C4=NC=NC(=C4)C#N | ||
Chemical Name | |||
Formula | C20H18F2N6O | M. Wt | 396.40 |
Purity | 98% | Storage | Store at 4-8°C |
Description | GSK547 (RIP1i, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo; exhibited a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963; reprogrammed TAMs toward an MHCIIhiTNFα+IFNγ+ immunogenic phenotype in a STAT1-dependent manner. RIP1 inhibition in TAMs resulted in cytotoxic T cell activation and T helper cell differentiation toward a mixed Th1/Th17 phenotype, leading to tumor immunity in mice and in organotypic models of human Pancreatic ductal adenocarcinoma (PDA). |
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