TOFA-RMI14514-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETOFACat. No.: HY-101068CAS No.: 54857-86-2Synonyms: RMI14514; MDL14514分式: CHO分量: 324.45作靶點: Acetyl-CoA Carboxylase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO

2、 : 34 mg/mL (104.79 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.71 mM); Suspended solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.71 mM); Suspended solution; Need ultrasonic3. 請

3、依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.71 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TOFA (RMI14514;MDL14514)酰輔酶A羧化酶- (ACCA )的變構抑制劑。體外研究 TOFA (5-tetradecyloxy-2-furoic acid) is cytotoxic to lung cancer cells NCI-H460 and colon carcinoma cellsHCT-8 and HCT-15, with an IC50 at approxim

4、ately 5.0, 5.0, and 4.5 g/mL, respectively. TOFA at 1.020.0 g/mL effectively blocks fatty acid synthesis and induces cell death in a dose-dependent manner 1. TOFA isfound to be cytotoxic to COC1 and COC1/DDP cells with IC50 values of 26.1 and 11.6 g/mL, respectively.TOFA inhibits the proliferation o

5、f the cancer cells examined in a time and dose dependent manner, arreststhe cells in the G0/G1 cell cycle phase and induces apoptosis 2. Acetyl-CoA-carboxylase- (ACCA) is a keyenzyme in the regulation of fatty acids synthesis. Inhibition of ACCA by TOFA decreases fatty acid synthesisand induces casp

6、ase activation and cell death in most PCa cell lines 3.體內研究 TOFA inhibits COC1/DDP cell growth in ovarian tumor mouse xenografts. The tumor growth rate issignificantly inhibited by TOFA compared with the DMSO treated control mice (1649356.3 vs. 5128390.4mm3. No toxicity is observed in the heart, liv

7、er, spleen, lung, kidney and intestinal tissues. By inhibiting ACC,TOFA may be a promising small molecule agent for ovarian cancer therapy 2.PROTOCOLCell Assay 1 NCI-H460, human lung cancer cells, and HCT-8 and HCT-15 cells (5,000/well) are seeded in 96-well platesovernight and then exposed to TOFA

8、at indicated concentrations (0, 1, 5, 10, 20, 50 g/mL) for 72 hours.Viable cells are detected using MTT assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are treated with 50 L DMSO (control group) or treated with TOFA (50 mg/kg).

9、 The drugs areAdministration 2 injected intraperitoneally daily for two weeks. Tumor volumes are recorded every two days by measuringdimensions (length and width) with Vernier calipers. The mice are sacrificed four weeks after the finaltreatment. Tumor weights are measured by a scale 2.MCE has not i

10、ndependently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. 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 growt

11、h 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-1and kills prostate cancer cells independent of p53 status. Cancer Biol Ther. 2011 Jul 1;12(1):80-5.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has no