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Limited Quantity USD 15-60
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 13710-19-5 Chemical Structure| 13710-19-5

Structure of Tolfenamic Acid
CAS No.: 13710-19-5

Chemical Structure| 13710-19-5

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Tolfenamic acid is a selective COX2 inhibitor with IC50 of 13.49 μM, it's a non-steroidal anti-inflammatory drugs (NSAIDs).

Synonyms: GEA 6414; Clotam

4.5 *For Research Use Only !

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Product Details of Tolfenamic Acid

CAS No. :13710-19-5
Formula : C14H12ClNO2
M.W : 261.70
SMILES Code : O=C(O)C1=CC=CC=C1NC2=CC=CC(Cl)=C2C
Synonyms :
GEA 6414; Clotam
MDL No. :MFCD00133865
InChI Key :YEZNLOUZAIOMLT-UHFFFAOYSA-N
Pubchem ID :610479

Safety of Tolfenamic Acid

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P501-P270-P264-P301+P310+P330-P405
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • COX-2

    COX-2, IC50:0.2 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
FG cells 2.5, 5.0, 10.0, 20.0, 40.0 μM TA 24-48 hours To evaluate the cytotoxicity of TA on FG cells, results showed dose-dependent inhibition of cell proliferation Cancer Res. 2010 Feb 1;70(3):1111-9.
PANC-1 cells 0.05 μM MIT + 5 μM TA 12 hours To evaluate the effect of combined MIT and TA on Sp1 protein expression, results showed significant downregulation of Sp1 protein expression Cancer Res. 2010 Feb 1;70(3):1111-9.
PANC-1 cells 5, 10, 20 μM 24 hours To evaluate the effect of TA on Sp1 protein expression, results showed dose-dependent downregulation of Sp1 protein expression Cancer Res. 2010 Feb 1;70(3):1111-9.
SKBR3 cells 25-100 µM 6 days Tolfenamic acid inhibited the proliferation of SKBR3 cells with an IC50 value of 52.5 µM. Mol Cancer Ther. 2009 May;8(5):1207-17.
BT474 cells 25-100 µM 6 days Tolfenamic acid inhibited the proliferation of BT474 cells with an IC50 value of 41.5 µM. Mol Cancer Ther. 2009 May;8(5):1207-17.
RD cells 100 μM 24 or 48 hours Inhibited cell proliferation and migration, induced apoptosis Int J Cancer. 2013 Feb 15;132(4):795-806.
RH30 cells 75 μM 24 or 48 hours Inhibited cell proliferation and migration, induced apoptosis Int J Cancer. 2013 Feb 15;132(4):795-806.
Schistosoma mansoni adult worms 50 μM 72 hours Evaluation of the schistosomicidal effect of Tolfenamic Acid on adult worms, LC50 of 20.6 μM. EBioMedicine. 2019 May;43:370-379.
SH-SY5Y cells 25 µM 72 hours To evaluate the inhibitory effects of TA and its analogs TN3 and TN7 on SP1-DNA binding. Results showed that TA, TN3, and TN7 all reduced SP1-DNA binding. Int J Mol Sci. 2023 Oct 16;24(20):15216.
SH-SY5Y neuroblastoma cells 25 μM and 50 μM 48 hours and 96 hours To investigate the effects of tolfenamic acid on Pb-induced SP1, APP, and Aβ levels. Results showed that tolfenamic acid significantly reduced Pb-induced SP1, APP, and Aβ levels. Neuropharmacology. 2014 Apr;79:596-602.
H9C2 myoblasts 50 μM 6 hours Inhibition of SP1 to mitigate Aβ-induced cell death and cardiomyocyte contractile dysfunction Acta Pharmacol Sin. 2022 Jan;43(1):39-49.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice BT474 cell mammary fat pad xenograft model Oral gavage 25 mg/kg/d Once daily for 27 days Tolfenamic acid significantly inhibited the growth of BT474 cell xenografts and reduced tumor weight. Mol Cancer Ther. 2009 May;8(5):1207-17.
Athymic nude mice RH30 cell xenograft model Oral gavage 50 mg/kg/dose Every second day for 20 days Inhibited tumor growth, downregulated Sp1, Sp3, Sp4 and Sp-regulated genes Int J Cancer. 2013 Feb 15;132(4):795-806.
APP YAC transgenic mice Alzheimer's disease model Oral gavage 5 mg/kg and 50 mg/kg Once daily for 34 days To investigate the effects of tolfenamic acid on BACE1 gene expression and enzyme activity. Results showed that tolfenamic acid significantly reduced BACE1 gene expression and enzyme activity. Neuropharmacology. 2014 Apr;79:596-602.
Female Swiss mice Schistosoma mansoni infection model Oral 400 mg/kg single dose Single dose Evaluation of the schistosomicidal effect of Tolfenamic Acid on adult worms in mice, worm burden reduction of 62.4%. EBioMedicine. 2019 May;43:370-379.
Transgenic mice Alzheimer's disease model Oral gavage 5 or 50 mg/kg Once daily for 34 days Tolfenamic acid lowers tau mRNA and protein, as well as the levels of its phosphorylated form and CDK5. J Neurochem. 2015 Apr;133(2):266-72
Mice AD transgenic mouse model Oral gavage 5 and 50 mg/kg/day Daily administration for 34 days To evaluate the cognitive improvement effects of tolfenamic acid, results showed that 50 mg/kg/day dose significantly improved long-term and working memory deficits. Neurobiol Aging. 2013 Oct;34(10):2421-30
Nude mice PANC-1 xenograft model Oral gavage 10 mg/kg Twice a week for 45 days To evaluate the effect of TA alone on tumor growth, results showed marginal antitumor activity at low doses Cancer Res. 2010 Feb 1;70(3):1111-9.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02159248 Pancreatic Cancer Phase 1 Withdrawn(The study closed pri... More >>or to enrolling any participants.) Less << December 2019 United States, Florida ... More >> UF Health Cancer Center at Orlando Health Orlando, Florida, United States, 32806 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.82mL

0.76mL

0.38mL

19.11mL

3.82mL

1.91mL

38.21mL

7.64mL

3.82mL

References

 

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