2226735-55-1
2226735-55-1 structure
- Name: GSK547
- Chemical Name: GSK547
- CAS Number: 2226735-55-1
- Molecular Formula: C20H18F2N6O
- Molecular Weight: 396.39
- Catalog: Signaling Pathways Apoptosis RIP kinase
- Create Date: 2019-06-02 10:12:50
- Modify Date: 2024-01-08 22:26:50
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GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
| Name | GSK547 |
|---|
| Description | GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1]. |
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| Related Catalog | |
| Target |
RIP1[1] |
| In Vitro | GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC50 of 32 nM after 24 hours[1]. GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)[1]. Cell Viability Assay[1] Cell Line: L929 cells (Mouse L-cells NCTC 929) Concentration: 0.1 nM; 10 nM; 1000 nM; 100000 nM Incubation Time: 24 hours Result: Reduced viability of L929 cells after co-treatment with TNFα and zVAD with an IC50 of 32 nM. Western Blot Analysis[1] Cell Line: Bone marrow-derived macrophages (BMDM) Concentration: Incubation Time: 30 minutes Result: Up-regulated STAT1 signaling in BMDM. |
| In Vivo | GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA)[1]. GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s[1]. Animal Model: The wild-type (WT) mice orthotopically implanted with Pdx1Cre;KrasG12D;Trp53R172H (KPC)-derived tumor cells[1] Dosage: ~100 mg/kg Administration: Fed via food-based dosing, daily, 15-50 days Result: Reduced tumor burden and extended survival. |
| References |
| Molecular Formula | C20H18F2N6O |
|---|---|
| Molecular Weight | 396.39 |