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Purity: ≥98%
Tolfenamic Acid (formerly GEA 6414; GEA6414; GEA-6414; Clotam), a non-steroidal anti-inflammatory drugs (NSAIDs), is a potent and selective COX-2 inhibitor with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 of 0.2 μM.
| ln Vitro |
Nonsteroidal anti-inflammatory drug tolfenamic acid (GEA 6414) selectively inhibits COX-2 in LPS-treated canine DH82 monocytes with an IC50 of 13.49 μM (3.53 μg/mL). macrophages, although COX-1 is unaffected [1]. At 100 μM, tolfenamic acid (GEA 6414) suppresses more than 70% of BE3, OE33, and SKGT5 cell viability. Another strong Sp protein inhibitor is tolfenamic acid (GEA 6414), which has the ability to lower Sp1 and Sp4 as well as stop the expression of c-Met in esophageal cancer cells BE3 and SKGT5 [2]. L3.6pl cells are subjected to a considerable downregulation of CENPF, KIF20A, LMNB1, MYB, SKP2, CCNE2, and DDIT3 gene expression in response to 50 μM tolfenamic acid (GEA 6414)[3].
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| ln Vivo |
In an esophageal tumor model generated by N-nitrosomethylbenzylamine (NMBA), tolfenamic acid (GEA 6414) at a dose of 50 mg/kg, three times a week, suppresses the formation and incidence of tumors. Rats treated with NMBA also showed decreased tumor volume and variety when given tolfenamic acid (GEA 6414) [2].
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| Animal Protocol |
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| 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.
[2]. Maliakal P, et al. Chemopreventive effects of tolfenamic acid against esophageal tumorigenesis in rats. Invest New Drugs. 2012 Jun;30(3):853-61. [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 |
| Molecular Formula |
C14H12CLNO2
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| Molecular Weight |
261.7
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| CAS # |
13710-19-5
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| Related CAS # |
Tolfenamic acid-d4;1246820-82-5;Tolfenamic acid-13C6;1420043-61-3
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| SMILES |
ClC1=C([H])C([H])=C([H])C(=C1C([H])([H])[H])N([H])C1=C([H])C([H])=C([H])C([H])=C1C(=O)O[H]
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| InChi Key |
YEZNLOUZAIOMLT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12ClNO2/c1-9-11(15)6-4-8-12(9)16-13-7-3-2-5-10(13)14(17)18/h2-8,16H,1H3,(H,17,18)
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| Chemical Name |
2-((3-chloro-2-methylphenyl)amino)benzoic acid
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| Synonyms |
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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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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8212 mL | 19.1058 mL | 38.2117 mL | |
| 5 mM | 0.7642 mL | 3.8212 mL | 7.6423 mL | |
| 10 mM | 0.3821 mL | 1.9106 mL | 3.8212 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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