GNF-6231
Catalog No.S8644
Molecular Weight(MW): 448.49
GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
Purity & Quality Control
Choose Selective Wnt/beta-catenin Inhibitors
Biological Activity
| Description | GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM. | ||
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| 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]. |
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| 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: |
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| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 89 mg/mL (198.44 mM) |
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| 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 |
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| Formula | C24H25FN6O2 |
| CAS No. | 1243245-18-2 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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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.
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