2. Immunology/Inflammation
  3. COX
  4. Tolfenamic Acid

トルフェナム酸  (Synonyms: Tolfenamic Acid)

製品番号: HY-B0335 純度: 99.94%
COA 取扱説明書 Technical Support

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.

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Tolfenamic Acid

トルフェナム酸 構造式

CAS 番号 : 13710-19-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 38 在庫あり
Solution
10 mM * 1 mL in DMSO USD 38 在庫あり
Solid
500 mg $35 在庫あり
5 g $64 在庫あり
10 g $110 在庫あり
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 2 publication(s) in Google Scholar

Other Forms of Tolfenamic Acid:

トルフェナム酸 関連抗体

Top Publications Citing Use of Products

COX アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
COX COX-1 COX-2 COX-3

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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.

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]
体外実験

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.

トルフェナム酸 関連抗体
体内実験

Tolfenamic Acid (GEA 6414) (50 mg/kg 3 times/wk, p.o.) inhibits tumor formation and tumor incidence in N-nitrosomethylbenzylamine (NMBA)-induced esophageal tumor model. Tolfenamic Acid (GEA 6414) also causes decreases in tumor multiplicity and tumor volume in rats treated with NMBA[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

261.70

分子式

C14H12ClNO2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=CC=C1NC2=C(C)C(Cl)=CC=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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: ≥ 2.08 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.
純度とドキュメンテーション

純度: 99.94%

COA (249 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[2]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[2]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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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Tolfenamic Acid Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Tolfenamic Acid13710-19-5GEA 6414GEA6414GEA-6414COXCyclooxygenaseInhibitorinhibitorinhibit

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