Home Apoptosis c-RET inhibitor GSK3179106

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GSK3179106 c-RET inhibitor

Cat.No.S8821

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 this compound is efficacious in vivo.
GSK3179106 c-RET inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 467.41

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (198.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
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Chemical Information, Storage & Stability

Molecular Weight 467.41 Formula

C22H21F4N3O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1627856-64-7 -- Storage of Stock Solutions

Synonyms N/A Smiles CCOC1=CC(=O)NC=C1C2=CC(=C(C=C2)CC(=O)NC3=NOC(=C3)C(C)(C)C(F)(F)F)F

Mechanism of Action

Targets/IC50/Ki
RET
(Cell-free assay)
0.3 nM
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.
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 this compound in the colon contents, jejunum, duodenum, and ileum, over that in plasma.
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02727283 Completed
Irritable Bowel Syndrome
GlaxoSmithKline
 November 26 2015 Phase 1

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