Home Stem Cells & Wnt PORCN inhibitor GNF-6231 For research use only.

GNF-6231

GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.

GNF-6231 Chemical Structure

GNF-6231 Chemical Structure

CAS No. 1243245-18-2

Purity & Quality Control

GNF-6231 Related Products

Biological Activity

Description GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
Targets
Porcupine [1]
(Cell-free)
0.8 nM
In vitro
In vitro GNF-6231 shows a good solubility. It has no appreciable activities, at least up to 10 μM testing concentrations, for more than 200 off-targets, which include GPCRs, kinases, proteases, transporters, ion channels, and nuclear receptors. GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested (2C9, 2D6, 3A4). It shows high permeability in a Caco-2 human cell permeability assay with a possible efflux[1].
Cell Research Cell lines TM3 Wnt-Luc cells and L-cell Wnt3A cells
Concentrations --
Incubation Time 24 h
Method

The TM3 Wnt-Luc cells and L-cell Wnt3A cells are cocultured in a 384-well plate with DMEM supplemented with 2% (vol/vol) FBS and treated with different concentrations of compounds. After 24 h, the firefly luciferase activities are assayed with the Bright-Glo Luciferase Assay System. The IC50 is measured when the effect of the compound reduces the luminescence signal by 50%. All compounds are tested in triplicates.
In Vivo
In vivo GNF-6231 demonstrates excellent pathway inhibition and induces robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model. GNF-6231 is moderately bound to mouse, rat, dog, monkey, and human plasma proteins (88.0, 83.1, 90.9, 71.2, and 95%, respectively). It shows good oral bioavailability, ranging from 72 to 96% in preclinical species (mouse, rat, and dog) when dosed in solution formulations. GNF-6231 is expected to have minimal to marginal distribution to tissues compared to total body water following intravenous administration to mouse (Vss 0.57 L/kg), rat (Vss 0.70 L/kg), and dog (Vss 0.25 L/kg)[1].
Animal Research Animal Models Nude mice
Dosages 3 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 448.49 Formula

C24H25FN6O2
CAS No. 1243245-18-2 SDF Download GNF-6231 SDF
Smiles CC1=CC(=CN=C1C2=CC(=NC=C2)F)CC(=O)NC3=NC=C(C=C3)N4CCN(CC4)C(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (198.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

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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