MF-766
Based on 1 Customer Validation
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1050656-06-8
- Formula: C27H21F3N2O3
- Molecular Weight:478.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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GPCR/G Protein Compound Library
HY-L006
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Immunology/Inflammation Compound Library
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HY-L025
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HY-L099
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Biological Activity
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EP4 0.23 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.3 nM
Compound: 9a, MF766
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Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay
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[PMID: 20471829] |
| HEK293 | IC50 |
1.8 nM
Compound: 9a, MF766
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Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
Antagonist activity at human prostanoid EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by scintillation proximity assay in presence of 10% human serum
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[PMID: 20471829] |
MF-766 (0.01-10 μM; pretreatment for 1 h and then stimulated with 50?ng/mL IL-2; with and without 0.33?μM PGE2; 18 hours) reverses PGE2-suppressed IFN-γ secretion in human NK cells. Additionally, NK cell viability is not affected by MF-766[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cells[2]
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Dosage:30 mg/kg combination with anti-PD-1 mDX400
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Administration:Oral gavage; 10 mg/kg or 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8
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Result:Improved anti-tumor activity in the setting of PD-1 blockade in multiple syngeneic models.
Chemical Information
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CAS No. 1050656-06-8
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Appearance Solid
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Molecular Weight 478.46
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Formula C27H21F3N2O3
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(C2(NC(C3=CC=CC4=C3N(CC5=CC=C(C(F)(F)F)C=C5)C=C4)=O)CC2)C=C1
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (104.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. John Colucci, et al. Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain. Bioorg Med Chem Lett [Content Brief]
[2]. Yun Wang, et al. Combination of EP 4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0900 mL | 10.4502 mL | 20.9004 mL | 52.2510 mL |
| 5 mM | 0.4180 mL | 2.0900 mL | 4.1801 mL | 10.4502 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0900 mL | 5.2251 mL | |
| 15 mM | 0.1393 mL | 0.6967 mL | 1.3934 mL | 3.4834 mL | |
| 20 mM | 0.1045 mL | 0.5225 mL | 1.0450 mL | 2.6125 mL | |
| 25 mM | 0.0836 mL | 0.4180 mL | 0.8360 mL | 2.0900 mL | |
| 30 mM | 0.0697 mL | 0.3483 mL | 0.6967 mL | 1.7417 mL | |
| 40 mM | 0.0523 mL | 0.2613 mL | 0.5225 mL | 1.3063 mL | |
| 50 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0450 mL | |
| 60 mM | 0.0348 mL | 0.1742 mL | 0.3483 mL | 0.8708 mL | |
| 80 mM | 0.0261 mL | 0.1306 mL | 0.2613 mL | 0.6531 mL | |
| 100 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5225 mL |
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