Tolfenamic Acid

目录号: GC15395纯度: >98.00%同义词: 托芬那酸; GEA 6414
An NSAID with anticancer activity

Tolfenamic Acid
Cas No.: 13710-19-5
规格价格库存数量操作
50mg¥326.00现货
1
10mM (in 1mL DMSO)¥357.00现货
1

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产品描述 Description

Tolfenamic Acid (GEA 6414) is a 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.

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].

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].

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

实验参考方法 Experimental Reference Method

Cell experiment:

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].

Animal experiment:

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].

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

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
13710-19-5
同义词
托芬那酸; GEA 6414
化学名
2-(3-chloro-2-methylanilino)benzoic acid
SMILES
CC1=C(C=CC=C1Cl)NC2=CC=CC=C2C(=O)O
分子式
C14H12ClNO2
分子量
261.7 g/mol
溶解性
≥ 13.085mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol