GNF-6231

Catalog No.S8644 Batch:S864402

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Technical Data

Formula

C24H25FN6O2
Molecular Weight 448.49 CAS No. 1243245-18-2
Solubility (25°C)* In vitro DMSO 89 mg/mL (198.44 mM)
Ethanol 5 mg/mL (11.14 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Nude mice

  • Dosages

    3 mg/kg

  • Administration

    by oral gavage

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.