TOFA (RMI14514)

A non-cytotoxic inhibitor of ACC and fatty acid synthesis

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5mg

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货号: ajce49672
CAS: 54857-86-2
别名: 5-(十四烷基氧)-2-糠酸,RMI14514; MDL14514
分子式: C19H32O4
分子量: 324.45
纯度: >98%
溶解度: DMSO : ≥ 34 mg/mL (104.79 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Inhibition of fatty acid synthase (FASN) by the irreversible inhibitor cerulenin leads to cytotoxicity and apoptosis in human cancer cell lines.¹ TOFA is an inhibitor of fatty acid synthesis blocking the synthesis of malonyl-CoA by acetyl-CoA carboxylase (ACC).² Both cerulenin (at about 10 ?g/ml) and TOFA (at about 1 ?g/ml) are effective at blocking the incorporation of radiolabeled acetate into palmitate. However, TOFA reduces malonyl-CoA levels rather than elevating them, and TOFA is relatively non-toxic to various cancer cell lines. TOFA also attenuates the inhibition of feeding observed when FASN inhibitors such as cerulenin and C75 are administered to obese ob/ob mice.

1.Moche, M., Schneider, G., Edwards, P., et al.Structure of the complex between the antibiotic cerulenin and its target, β-ketoacyl-acyl carrier protein synthaseJ. Biol. Chem.274(10)6031-6034(1999) 2.Loftus, T.M., Jaworsky, D.E., Frehywot, G.L., et al.Reduced food intake and body weight in mice treated with fatty acid synthase inhibitorsScience2882379-2381(2000)

Protocol

Cell experiment:

NCI-H460, human lung cancer cells, and HCT-8 and HCT-15 cells (5,000/well) are seeded in 96-well plates overnight and then exposed to TOFA at indicated concentrations (0, 1, 5, 10, 20, 50 μg/mL) for 72 hours. Viable cells are detected using MTT assay[1].

Animal experiment:

Mice: Mice are treated with 50 μL DMSO (control group) or treated with TOFA (50 mg/kg). The drugs are injected intraperitoneally daily for two weeks. Tumor volumes are recorded every two days by measuring dimensions (length and width) with Vernier calipers. The mice are sacrificed four weeks after the final treatment. Tumor weights are measured by a scale[2].

参考文献:

[1]. Wang C, et al. Acetyl-CoA carboxylase-alpha inhibitor TOFA induces human cancer cell apoptosis. Biochem Biophys Res Commun. 2009 Jul 31;385(3):302-6.
[2]. Li S, et al. TOFA suppresses ovarian cancer cell growth in vitro and in vivo. Mol Med Rep. 2013 Aug;8(2):373-8.
[3]. Guseva NV, et al. TOFA (5-tetradecyl-oxy-2-furoic acid) reduces fatty acid synthesis, inhibits expression of AR, neuropilin-1 and Mcl-1 and kills prostate cancer cells independent of p53 status. Cancer Biol Ther. 2011 Jul 1;12(1):80-5.