For research use only.

Catalog No.S8787

GSK'547 Chemical Structure

CAS No. 2226735-55-1

GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963

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Choose Selective RIP kinase Inhibitors

Biological Activity

Description GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
RIP1 [1]
In vitro

GSK'547 (RIP1i) treatment in vitro directs the programming of bone marrow-derived macrophages (BMDM) toward an immunogenic phenotype, upregulating MHC-II, TNFa, and IFNg, while concomitantly reducing CD206, IL-10, and TGFb expression. Moreover, RIP1i upregulates STAT1 signaling in BMDM, which is associated with M1 programming, but reduced STAT3, STAT5, and STAT6 signaling, which are linked to M2-like macrophage differentiation. Furthermore, RIP1i-treated macrophages display enhanced ability to capture antigen[1].

In vivo

Administration of GSK'547 (RIP1i) in mouse chow achieves in vivo steady-state concentrations above the L929 IC90 over a 24-hr period. High serum concentrations of RIP1i are sustained over a 6-week treatment course. RIP1i treatment is well tolerated without evident pathology. In mice challenged with orthotopic PDA (pancreatic ductal adenocarcinoma) tumor cells derived from KPC mice, RIP1i reduces tumor burden and extends survival cpmpared with mice treated with controls or Nec-1s. RIP1i also protects against established tumors and liver metastases[1].


Cell Research:


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  • Cell lines: L929 cells
  • Concentrations: --
  • Incubation Time: 30 min
  • Method:

    Cells are pretreated with RIP1i at various doses for 30 min. Induced cell death is evaluated 24 hr later by measuring cellular ATP levels.

    (Only for Reference)
Animal Research:


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  • Animal Models: C57BL/6 mice
  • Dosages: 100 mg/kg/day
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 29 mg/mL (73.16 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.39


CAS No. 2226735-55-1
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(CCC1C(=O)N2C(CC=N2)C3=CC(=CC(=C3)F)F)C4=NC=NC(=C4)C#N

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01199250 Not yet recruiting Other: Laboratory Biomarker Analysis Lynch Syndrome|Recurrent Uterine Corpus Carcinoma|Stage I Uterine Corpus Cancer|Stage II Uterine Corpus Cancer|Stage III Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer Gynecologic Oncology Group|National Cancer Institute (NCI) January 2100 --
NCT04151225 Withdrawn Drug: GSK2330811|Drug: Placebo Crohns Disease GlaxoSmithKline April 5 2021 Phase 2
NCT04676516 Not yet recruiting Drug: GSK3326595 Breast Cancer Ottawa Hospital Research Institute|Ontario Institute for Cancer Research|GlaxoSmithKline|London Regional Cancer Program Canada|Hamilton Health Sciences Corporation December 21 2020 Phase 2
NCT04654143 Recruiting Drug: BVL-GSK098 capsule placebo Healthy Volunteers BioVersys AG December 2 2020 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID