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
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-14398
CelecoxibCOX-2inhibitor -
HY-B1320
Meclofenamic acid sodiumFTO Inhibitor -
HY-15036
DiclofenacCOX Inhibitor -
HY-B1221
Flufenamic acidCOX Inhibitor -
HY-B0574
Mefenamic acidCOX Inhibitor -
HY-14397
IndomethacinCOX1/2 Inhibitor -
HY-B0335R
Tolfenamic Acid (Standard)COX-2 Inhibitor -
HY-B0223
AlbendazoleParasiticide -
HY-76251
EtodolacCOX Inhibitor -
HY-78131
IbuprofenCOX-1 Inhibitor -
HY-B0634
AceclofenacNSAID -
HY-14872
TideglusibGSK-3 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Tolfenamic Acid
More
Biological Activity
Description
IC50 & Target
[1]|
COX-2 13.49 μM (IC50, in cell) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| C6 | IC50 |
>100 μM
Compound: Tolfenamic acid
|
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
|
[PMID: 34537445] |
| CT26.WT | IC50 |
>100 μM
Compound: TA
|
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
|
[PMID: 35868003] |
| D283 Med | IC50 |
20.8 μg/mL
Compound: Tolfenamic acid
|
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
|
[PMID: 33636537] |
| Daoy | IC50 |
21.6 μg/mL
Compound: Tolfenamic acid
|
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
|
[PMID: 33636537] |
| HGC-27 | IC50 |
>100 μM
Compound: TA
|
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
|
[PMID: 35868003] |
| HT-29 | IC50 |
>100 μM
Compound: TA
|
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
|
[PMID: 35868003] |
| RKO | IC50 |
>100 μM
Compound: TA
|
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
|
[PMID: 35868003] |
| SGC-7901 | IC50 |
>100 μM
Compound: TA
|
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
|
[PMID: 35868003] |
| U-251 | IC50 |
>100 μM
Compound: Tolfenamic acid
|
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
|
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
|
[PMID: 34537445] |
In Vitro
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 13710-19-5
-
Appearance Solid
-
Molecular Weight 261.70
-
Formula C14H12ClNO2
-
Color White to off-white
-
SMILES
O=C(O)C1=CC=CC=C1NC2=C(C)C(Cl)=CC=C2
-
Synonyms
GEA 6414
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
In Vitro:
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)
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
-
Data Sheet (282 KB)
-
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)
-
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 |
Tolfenamic Acid Related Classifications
HY-B0335 Related Classifications
Powered by Bioz