Home Apoptosis c-RET inhibitor GSK3179106 For research use only.

GSK3179106

GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.

GSK3179106 Chemical Structure

GSK3179106 Chemical Structure

CAS No. 1627856-64-7

Purity & Quality Control

Batch: S882101 DMSO]93 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

GSK3179106 Related Products

Signaling Pathway

c-RET Signaling Pathways

c-RET Signaling Pathway

Biological Activity

Description GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.
Targets
RET [1]
(Cell-free assay)
0.3 nM
In vitro
In vitro

GSK3179106 has a clean genotoxic profile with no embedded genotoxicity liabilities and possesses good kinase selectivity: only 26 out of a set of >300 recombinant kinases are found to be inhibited at a 1 μM test concentration[1].
In Vivo
In vivo

Single dose IV (bolus, 0.06 mg/kg) PK in male Sprague-Dawley rats of compound GSK3179106 formulated as 0.04 mg/mL in DMSO/6% HP-beta-CD = 5:95 with a pH of 7 as a clear solution shows low exposure with an AUC of 102 ng·h/mL. Oral PK is evaluated with the same dosing regimen as the in vivo colonic hypersensitivity model, seven doses of 10 mg/kg given over 3.5 days. Full gut PK measurements are also taken to help understand the PK/PD relationship--It reveals high concentrations of GSK3179106 in the colon contents, jejunum, duodenum, and ileum, over that in plasma[1].
Animal Research Animal Models male Sprague-Dawley rats
Dosages 0.06 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02727283 Completed
Irritable Bowel Syndrome
GlaxoSmithKline
 November 26 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 467.41 Formula

C22H21F4N3O4
CAS No. 1627856-64-7 SDF --
Smiles CCOC1=CC(=O)NC=C1C2=CC(=C(C=C2)CC(=O)NC3=NOC(=C3)C(C)(C)C(F)(F)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (198.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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