Home Apoptosis RIP kinase inhibitor GSK'547 For research use only.

GSK'547

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

GSK'547 Chemical Structure

GSK'547 Chemical Structure

CAS: 2226735-55-1

Selleck's GSK'547 has been cited by 1 publication

Purity & Quality Control

Batch: S878701 DMSO] 29 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.86%
99.86

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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
Targets
RIP1 [1]
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 100 mg/kg/day
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01199250 Not yet recruiting
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)|GOG Foundation
 January 2100 --
NCT06104319 Not yet recruiting
Non-alcoholic Fatty Liver Disease
GlaxoSmithKline
 January 9 2024 Phase 2
NCT06188507 Not yet recruiting
Systemic Lupus Erythematosus
GlaxoSmithKline
 January 11 2024 Phase 1
NCT06171113 Not yet recruiting
Malaria Falciparum
GlaxoSmithKline
 December 12 2023 Phase 1
NCT06154837 Not yet recruiting
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 November 27 2023 Phase 1
NCT05999799 Recruiting
Dermatitis Atopic
GlaxoSmithKline
 November 15 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 396.39 Formula

C20H18F2N6O
CAS No. 2226735-55-1 SDF --
Smiles C1CN(CCC1C(=O)N2C(CC=N2)C3=CC(=CC(=C3)F)F)C4=NC=NC(=C4)C#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 29 mg/mL ( (73.16 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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