Tolfenamic Acid (Synonyms: GEA 6414)

Name: Tolfenamic Acid
Brand: MedChemExpress
SKU: HY-B0335
Rating: 5.0 (2 reviews)

Cat. No.: HY-B0335 Purity: 99.94%: Data Sheet
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Handling Instructions
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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 화학구조

CAS No. : 13710-19-5

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
500 mg	해외재고보유	Estimated Time of Arrival: December 31
5 g	해외재고보유	Estimated Time of Arrival: December 31
10 g	해외재고보유	Estimated Time of Arrival: December 31
50 g	견적 받기

or 대량구매 문의

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

고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Tolfenamic Acid:

2 Publications Citing Use of MCE Tolfenamic Acid

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•Related Screening Libraries:

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View All COX Isoform Specific Products:

View All Isoforms

COX COX-1 COX-2 COX-3

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

COX-2

13.49 μM (IC₅₀, in cell)

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	>100 3 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]
C6	IC₅₀	> 100 3 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 3 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 6 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]
CT26.WT	IC₅₀	> 100 3 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]
Daoy	IC₅₀	21.6 6 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 3 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]
D283 Med	IC₅₀	20.8 6 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]
HT-29	IC₅₀	>100 3 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 3 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]
Daoy	IC₅₀	21.6 6 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 3 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]
SGC-7901	IC₅₀	>100 3 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]
HT-29	IC₅₀	> 100 3 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]
U-251	IC₅₀	>100 3 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 3 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]
RKO	IC₅₀	> 100 3 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 3 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 3 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 3 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.

In Vivo

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.

Clinical Trial

분자량

261.70

화학식

C₁₄H₁₂ClNO₂

CAS No.

13710-19-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=CC=C1NC2=C(C)C(Cl)=CC=C2

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

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.

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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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

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(per animal)

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.

순도&문서

Purity: 99.94%

Select Batch:

Data Sheet (282 KB) SDS (480 KB)

COA (249 KB) LCMS (95 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]

Cell Assay ^[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]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[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]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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

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

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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Tolfenamic Acid (Synonyms: GEA 6414)

고객리뷰

Other Forms of Tolfenamic Acid:

Tolfenamic Acid Related Antibodies

2 Publications Citing Use of MCE Tolfenamic Acid

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All COX Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Tolfenamic Acid Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Tolfenamic Acid Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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