GSK3145095

Catalog No.S8845

For research use only.

GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.

GSK3145095 Chemical Structure

CAS No. 1622849-43-7

Purity & Quality Control

Choose Selective RIP kinase Inhibitors

Biological Activity

Description GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
Targets
RIP1 kinase [1]
(Cell-free assay)
6.3 nM
In vitro

GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinasedependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor is also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: U937 cells, L-cells NCTC 929 (L929) cells
  • Concentrations: 0-3 μM
  • Incubation Time: 5 h
  • Method:

    GSK3145095 is prepared in assay buffer and serially diluted 1:1.5 in a 22 point titration (high final concentration 3 μM) and added to a 384 white low volume Greiner plate. 3.5 μL of each inhibitor concentration and 3.5 μL of 25 nM enzyme (final) in assay buffer are added to the plate. Following these additions, 3.5 μL of ATP (15.6 μM to 875 μM final) in assay buffer is added to the plate to initiate the reaction. The reaction progresses for 5h at room temperature.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 397.38
Formula

C20H17F2N5O2

CAS No. 1622849-43-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2=C(C(=CC(=C2)F)F)NC(=O)C1NC(=O)C3=NNC(=N3)CC4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

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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.

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.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03681951 Terminated Drug: GSK3145095|Drug: Pembrolizumab Neoplasms Pancreatic GlaxoSmithKline|Parexel November 16 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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