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Tolfenamic Acid

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Chemical Structure| 13710-19-5 同义名 : 托芬那酸 ;GEA 6414;Clotam
CAS号 : 13710-19-5
货号 : A127860
分子式 : C14H12ClNO2
纯度 : 98%
分子量 : 261.704
MDL号 : MFCD00133865
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(401.22 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX-2

    COX-2, IC50:0.2 μM
描述 Tolfenamic Acid 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[3]. Tolfenamic Acid also acts as a potent Sp protein inhibitor. Tolfenamic acid (TA) inhibits cancer cell proliferation and tumor growth through the degradation of Sp1, Sp3, and Sp4. Tolfenamic Acid (50 mg/kg 3 times/wk, p.o.) inhibits tumor formation and tumor incidence in N-nitrosomethylbenzylamine (NMBA)-induced esophageal tumor model. Tolfenamic Acid also causes decreases in tumor multiplicity and tumor volume in rats treated with NMBA[4]. Tolfenamic Acid (50 μM) significantly affects gene expression in L3.6pl cells, and downregulates CENPF, KIF20A, LMNB1, MYB, SKP2, CCNE2, and DDIT3[5]. TA has shown excellent in vitro antibacterial activity against certain ATCC strains of bacteria when complexed with bismuth(III) [6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02159248 Pancreatic Cancer Phase 1 Withdrawn(The study closed pri... 展开 >>or to enrolling any participants.) 收起 << December 2019 United States, Florida ... 展开 >> UF Health Cancer Center at Orlando Health Orlando, Florida, United States, 32806 收起 <<
实验方案
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
参考文献

[1]Sankpal UT, Goodison S, et al. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017 Feb 28;8(9):14593-14603.

[2]Lee SH, Bahn JH, et al. ESE-1/EGR-1 pathway plays a role in tolfenamic acid-induced apoptosis in colorectal cancer cells. Mol Cancer Ther, 2008. 7(12): p. 3739-50.

[3]Kay-Mugford P, Benn SJ, LaMarre J, Conlon P. In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs. Am J Vet Res. 2000;61(7):802-810

[4]Maliakal P, Abdelrahim M, Sankpal UT, et al. Chemopreventive effects of tolfenamic acid against esophageal tumorigenesis in rats. Invest New Drugs. 2012;30(3):853-861

[5]Sankpal UT, Goodison S, Jones-Pauley M, Hurtado M, Zhang F, Basha R. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017;8(9):14593-14603

[6]Ahmed S, Sheraz MA, Ahmad I. Tolfenamic Acid. Profiles Drug Subst Excip Relat Methodol. 2018;43:255-319