GNF-6231

Catalog No.S8644

GNF-6231 Chemical Structure

Molecular Weight(MW): 448.49

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

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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

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].

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].

Protocol

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Nude mice
  • Formulation: 20% (vol/vol) PEG300 and 30% (vol/vol) 10% ETPGS in water
  • Dosages: 3 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (198.44 mM)
Ethanol 5 mg/mL (11.14 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 448.49
Formula

C24H25FN6O2

CAS No. 1243245-18-2
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID