2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. MF-766

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.

MF-766 Chemical Structure

MF-766 Chemical Structure

CAS No. : 1050656-06-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 235 In-stock
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5 mg USD 220 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

MF-766 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2].

IC50 & Target[1]

EP4

0.23 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
1.3 nM
Compound: 9a, MF766
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
[PMID: 20471829]
HEK293 IC50
1.8 nM
Compound: 9a, MF766
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
[PMID: 20471829]
In Vitro

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.

MF-766 Related Antibodies
In Vivo

MF-766 (oral gavage; 30 mg/kg; once daily; 21 days) exhibits TGI% of 49% in CT26 tumor model. But it does not exhibits significant difference in EMT6 and 4T1 tumor model[2].
MF-766 (oral gavage; 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8) shows potent anti-tumor activities in different preclinical models. The % of TGI are 89%, 66% and 40%, respectively in CT26 tumor, EMT6 and 4T1 tumor model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cells[2]
Dosage: 30 mg/kg combination with anti-PD-1 mDX400
Administration: Oral gavage; 10 mg/kg or 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8
Result: Improved anti-tumor activity in the setting of PD-1 blockade in multiple syngeneic models.
Molecular Weight

478.46

Formula

C27H21F3N2O3
CAS No.
Appearance

Solid

Color

Off-white to gray

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0900 mL 10.4502 mL 20.9004 mL
5 mM 0.4180 mL 2.0900 mL 4.1801 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.69%

SDS (251 KB)

COA (249 KB) HNMR (102 KB) LCMS (225 KB)

Handling Instructions (2659 KB)
References

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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MF-766 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MF-7661050656-06-8MF766MF 766Prostaglandin ReceptorEP4cancerinflammation diseaseAIAarthritisanti-tumorInhibitorinhibitorinhibit

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