Tolfenamic Acid
Based on 2 publication(s) in Google Scholar
Tolfenamic Acid (GEA 6414) is a CNS-penetrant non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 13710-19-5
- Formula: C14H12ClNO2
- Molecular Weight:261.70
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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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tolfenamic Acid
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Biological Activity
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COX-2 13.49 μM (IC50, in cell) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C6 | IC50 |
>100 μM
Compound: Tolfenamic acid
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Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 34537445] |
| CT26.WT | IC50 |
>100 μM
Compound: TA
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Antiproliferative activity against mouse CT26.WT cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse CT26.WT cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 35868003] |
| D283 Med | IC50 |
20.8 μg/mL
Compound: Tolfenamic acid
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Antitumor activity against human D283 Med cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
Antitumor activity against human D283 Med cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 33636537] |
| Daoy | IC50 |
21.6 μg/mL
Compound: Tolfenamic acid
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Antitumor activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
Antitumor activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 33636537] |
| HGC-27 | IC50 |
>100 μM
Compound: TA
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Antiproliferative activity against human HGC-27 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 35868003] |
| HT-29 | IC50 |
>100 μM
Compound: TA
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Antiproliferative activity against human HT-29 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 35868003] |
| RKO | IC50 |
>100 μM
Compound: TA
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Antiproliferative activity against human RKO cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 35868003] |
| SGC-7901 | IC50 |
>100 μM
Compound: TA
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Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 35868003] |
| U-251 | IC50 |
>100 μM
Compound: Tolfenamic acid
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Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 34537445] |
| U-87MG ATCC | IC50 |
>100 μM
Compound: Tolfenamic acid
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Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 34537445] |
Tolfenamic Acid (GEA 6414) is a nonsteroidal antiinflammatory agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1[1].
Tolfenamic Acid (GEA 6414) (100 μM) inhibits >70% of cell viability of BE3, OE33, and SKGT5. Tolfenamic Acid (GEA 6414) also acts as a potent Sp protein inhibitor, decreases Sp1 and Sp4 and suppresses c-Met expression in esophageal cancer cells BE3 and SKGT5[2].
Tolfenamic AcidTolfenamic Acid (GEA 6414) (50 μM) significantly affects gene expression in L3.6pl cells, and downregulates CENPF, KIF20A, LMNB1, MYB, SKP2, CCNE2, and DDIT3[3].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 13710-19-5
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Appearance Solid
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Molecular Weight 261.70
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Formula C14H12ClNO2
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Color White to off-white
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SMILES
O=C(O)C1=CC=CC=C1NC2=C(C)C(Cl)=CC=C2
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Synonyms
GEA 6414
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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
Publications (2)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Neurosci Lett
2019 Mar 23:696:67-73. PMID: 30528877
Solvent & Solubility
DMSO : ≥ 100 mg/mL (382.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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.
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.
Protocol
All cells are grown in media (RPMI1640) supplemented with 5% serum and cultured at 37°C in a humidified atmosphere of 95% air and 5% CO2. Twenty four hours after seeding, cells are treated with vehicle (0.1% DMSO) or various concentrations of Tolfenamic Acid (GEA 6414) (25/50/100 μM). Cell viability assays are conducted at 24, 48 and 72 h post-treatment. Cells are treated with 50 μM Tolfenamic Acid (GEA 6414) and the cell pellets are harvested at 48 h post-treatment. These pellets are used to prepare cell lysates that are used in Western blot analyses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
The Fischer 344 (F-344) rat model of esophageal SCC are initially housed two per cage, but eventually separated to one per cage due to increase in size, and are maintained under standard, humane conditions (20±2°C, 50±10% relative humidity, 12-h light/dark cycles). Food and water are provided ad libitum. Body weights are recorded at the time of each dosing. Two weeks after arrival in the animal facility, the rats are randomLy assigned into 4 groups: C: NMBA (1-5 week); NTA: (NMBA 1-5 week and then Tolfenamic Acid (GEA 6414) 6-25 week); NC: Negative control (vehicle); and TA: Tolfenamic Acid (GEA 6414) negative control. Control (C) and NTA groups are injected s.c. with NMBA (0.5 mg/kg) in 0.2 mL vehicle three times per week for 5 weeks while negative control groups are injected with vehicle alone. NTA and Tolfenamic Acid groups also receive 50 mg/kg Tolfenamic Acid (GEA 6414) by oral gavage from week 6 through week 25. After the 25th week, the animals are sacrificed, esophagi are cut open longitudinally, and surface tumors are mapped and counted. The number and the size of lesions, including polyps are recorded and images captured. Tumor volume is calculated using the formula for a prolate spheroid: length × width × height × p/6[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Kay-Mugford P, et al. In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs. Am J Vet Res. 2000 Jul;61(7):802-10. [Content Brief]
[2]. Maliakal P, et al. Chemopreventive effects of tolfenamic acid against esophageal tumorigenesis in rats. Invest New Drugs. 2012 Jun;30(3):853-61. [Content Brief]
[3]. Sankpal UT, et al. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017 Feb 28;8(9):14593-14603 [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 | 3.8212 mL | 19.1058 mL | 38.2117 mL | 95.5292 mL |
| 5 mM | 0.7642 mL | 3.8212 mL | 7.6423 mL | 19.1058 mL | |
| 10 mM | 0.3821 mL | 1.9106 mL | 3.8212 mL | 9.5529 mL | |
| 15 mM | 0.2547 mL | 1.2737 mL | 2.5474 mL | 6.3686 mL | |
| 20 mM | 0.1911 mL | 0.9553 mL | 1.9106 mL | 4.7765 mL | |
| 25 mM | 0.1528 mL | 0.7642 mL | 1.5285 mL | 3.8212 mL | |
| 30 mM | 0.1274 mL | 0.6369 mL | 1.2737 mL | 3.1843 mL | |
| 40 mM | 0.0955 mL | 0.4776 mL | 0.9553 mL | 2.3882 mL | |
| 50 mM | 0.0764 mL | 0.3821 mL | 0.7642 mL | 1.9106 mL | |
| 60 mM | 0.0637 mL | 0.3184 mL | 0.6369 mL | 1.5922 mL | |
| 80 mM | 0.0478 mL | 0.2388 mL | 0.4776 mL | 1.1941 mL | |
| 100 mM | 0.0382 mL | 0.1911 mL | 0.3821 mL | 0.9553 mL |
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