Molecular Formula | C20H18F2N6O |
Molar Mass | 396.39 |
Density | 1.43±0.1 g/cm3(Predicted) |
Boling Point | 578.3±60.0 °C(Predicted) |
Solubility | DMSO : 100 mg/mL (252.28 mM; Need ultrasonic) |
pKa | 1.93±0.28(Predicted) |
Storage Condition | -20°C |
In vitro study | In Vitro, GSK'547 treatment directed bone marrow-derived macrophages to develop an immunogenic phenotype with upregulated expression of MHC-II, TNFa, and IFNg, while decreasing expression of CD206, IL-10, and TGFb. In addition, GSK'547 also upregulated STAT1 signaling and decreased STAT3, STAT5, and STAT6 signaling in bone marrow-derived macrophages. Macrophages treated with GSK'547 had a stronger ability to capture antigens. |
In vivo study | Mice were dosed with GSK'547 via food, and the concentration of GSK'547 in vivo was at a stable level for 24 hours, higher than the IC50 value in L929 cells. High levels of GSK'547 were maintained in vivo during administration for 6 weeks. GSK'547 was well tolerated with no apparent pathological features. In mice with pancreatic ductal adenocarcinoma in situ, GSK'547 reduced their tumor burden and prolonged survival compared to control and Nec-1s treated groups. GSK'547 protects against established tumors and liver metastases. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.523 ml | 12.614 ml | 25.228 ml |
5 mM | 0.505 ml | 2.523 ml | 5.046 ml |
10 mM | 0.252 ml | 1.261 ml | 2.523 ml |
5 mM | 0.05 ml | 0.252 ml | 0.505 ml |
biological activity | GSK'547 is a highly selective and potent RIP1 (RIPK1) inhibitor, in a mouse pharmacokinetic study, the oral exposure was increased 400-fold compared to GSK' 963. |
Target | Value |