GNF-6231
Based on 1 Customer Validation
GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1243245-18-2
- Formula: C24H25FN6O2
- Molecular Weight:448.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
GNF-6231 (0.3-3 mg/kg; p.o.; once daily for 2 weeks) shows antitumor activity in a mouse of MMTV-WNT1 xenograft tumor[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 mice model of myocardial infarction[1]
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Dosage:5 mg/kg
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Administration:Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours
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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.
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Animal Model:Mouse MMTV-WNT1 xenograft tumor model[2]
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Dosage:0.3 mg/kg,1.0 mg/kg, 3 mg/kg
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Administration:Oral gavage; Once daily for 2 weeks
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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.
Chemical Information
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CAS No. 1243245-18-2
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Appearance Solid
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Molecular Weight 448.49
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Formula C24H25FN6O2
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Color White to off-white
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SMILES
O=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
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.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.69 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.69 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bastakoty, Dikshya et al. Temporary, Systemic Inhibition of the WNT/β-Catenin Pathway promotes Regenerative Cardiac Repair following Myocardial Infarct. Cell, stem cells and regenerative medicine vol. 2,2 (2016): 10.16966/2472-6990.111. [Content Brief]
[2]. Kang, Sheng. Low-density lipoprotein receptor-related protein 6-mediated signaling pathways and associated cardiovascular diseases: diagnostic and therapeutic opportunities. Human genetics vol. 139,4 (2020): 447-459. [Content Brief]
[3]. Raeisi, Mortaza et al. Porcn as a novel therapeutic target in cancer therapy: A review. Cell biology international vol. 46,12 (2022): 1979-1991. [Content Brief]
[4]. Cheng, Dai et al. Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors. ACS medicinal chemistry letters vol. 7,7 676-80. 10 May. 2016, [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2297 mL | 11.1485 mL | 22.2970 mL | 55.7426 mL |
| 5 mM | 0.4459 mL | 2.2297 mL | 4.4594 mL | 11.1485 mL | |
| 10 mM | 0.2230 mL | 1.1149 mL | 2.2297 mL | 5.5743 mL | |
| 15 mM | 0.1486 mL | 0.7432 mL | 1.4865 mL | 3.7162 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1149 mL | 2.7871 mL | |
| 25 mM | 0.0892 mL | 0.4459 mL | 0.8919 mL | 2.2297 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8581 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3936 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1149 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 80 mM | 0.0279 mL | 0.1394 mL | 0.2787 mL | 0.6968 mL |
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