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GSK'547 RIP kinase inhibitor

Name: GSK'547
Brand: Selleck Chemicals
SKU: S8787
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8787

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

Chemical Structure

Molecular Weight: 396.39

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.86

Related Targets	Apoptosis related Ras STAT TNF-alpha Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 c-RET MDM2/MDMX Myc IAP OXPHOS PERK FKBP Thymidylate Synthase ABC Transporter Heme Oxygenase PFKFB Pyroptosis PKD Survivin ASK Bcl-6 Nur77 DAPK TRADD TACE Cuproptosis
Related Products	Necrostatin-1 (Nec-1) GSK872 Necrostatin 2 racemate (Nec-1s) Mito-TEMPO RIPA-56 GSK2982772 GSK'963 GSK583 GSK2983559 (compound 3) Resibufogenin ICCB-19 hydrochloride HS-1371 GSK481 RIP3 Antibody [J24B17] GSK2983559 active metabolite RIP Antibody [N10M19] RIP Antibody [P3C6] PK68 GSK-872 hydrochloride RIP3 Antibody [H22B6] GSK3145095 RIP2 Antibody [M23E23] Phospho-RIP3 (Ser232) Antibody [E19K17] Necrostatin-34 (Nec-34) Oditrasertib RIPK1-IN-7 OD36 GSK-843

Chemical Information, Storage & Stability

Molecular Weight	396.39	Formula	C₂₀H₁₈F₂N₆O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2226735-55-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCC1C(=O)N2C(CC=N2)C3=CC(=CC(=C3)F)F)C4=NC=NC(=C4)C#N

Solubility

In vitro
Batch:

DMSO : 29 mg/mL (73.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.45mg/ml (3.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 29 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.096mg/ml (0.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 1.92 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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].
References	[1] https://pubmed.ncbi.nlm.nih.gov/30423296/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	--
NCT06339034	Not yet recruiting	Parkinson Disease	State University of New York at Buffalo\|The Cure Parkinson''s Trust	June 2024	Phase 1\|Phase 2
NCT06317285	Not yet recruiting	Idiopathic Pulmonary Fibrosis	GlaxoSmithKline	April 1 2024	Phase 2
NCT06104319	Recruiting	Non-alcoholic Fatty Liver Disease	GlaxoSmithKline	January 22 2024	Phase 2
NCT06188507	Not yet recruiting	Systemic Lupus Erythematosus	GlaxoSmithKline	January 11 2024	Phase 1

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