| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H25FN6O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GNF-6231 is an orally active inhibitor of porcupine (IC50 = 0.8 nM), Pron, and an endoplasmic reticulum protein, and it has anticancer activity. It can prevent activation of the Wnt pathway by blocking secretion of all Wnt ligands, and it can be used in the study of myocardial infarction[1][2][3][4]. It is supplied as a white to off-white solid (C24H25FN6O2, MW 448.49) at 99.63% purity.
Physical & Chemical Properties
| CAS Number | 1243245-18-2 |
|---|---|
| Molecular Formula | C24H25FN6O2 |
| Molecular Weight | 448.49 g/mol |
| Purity | 99.63% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3 |
| Signaling Pathway | Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: ≥ 36 mg/mL (80.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 36 mg/mL (80.27 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 3 mg/mL (6.69 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (30.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 3 mg/mL (6.69 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (30.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 3 mg/mL (6.69 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (30.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
GNF-6231 inhibits Porcupine enzyme activity with an IC50 of 0.8 nM and is not cytotoxic across a concentration range of 20 μM[1].
In Vivo
In C57Bl/6 mice, GNF-6231 (5 mg/kg, i.v. injection; once every 24 hours for 6 days) alleviates myocardial infarction symptoms by inhibiting activation of the Wnt pathway[1]. In a mouse MMTV-WNT1 xenograft tumor model, GNF-6231 (0.3-3 mg/kg; p.o.; once daily for 2 weeks) exhibits antitumor activity[4].
| Animal Model | C57Bl/6 mice model of myocardial infarction[1] |
|---|---|
| Dosage | 5 mg/kg |
| Administration | Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours |
| Result | Reduced nuclear and cytoplasmic β-catenin levels. Reduced adverse cardiac remodeling and reduced myocardial infarction area in mice (9.07%). Enhanced the overall heart repair and recovery after left ventricular infarction. |
| Animal Model | Mouse MMTV-WNT1 xenograft tumor model[2] |
|---|---|
| Dosage | 0.3 mg/kg,1.0 mg/kg, 3 mg/kg |
| Administration | Oral gavage; Once daily for 2 weeks |
| Result | At a single dose of 3 mg/kg, reduced the level of Wnt target gene Axin2 mRNA. Promoted tumor regression in mice in a dose-dependent manner. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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