生物活性 | |||
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描述 | Acetyl-CoA carboxylase-alpha (ACCA) is a rate-limiting enzyme in long chain fatty acid synthesis, playing a critical role in cellular energy storage and lipid synthesis. TOFA (5-tetradecyloxy-2-furoic acid), an allosteric inhibitor of ACCA, is cytotoxic to lung cancer cells NCI-H460 and colon carcinoma cells HCT-8 and HCT-15, with IC50s at approximately 5.0, 5.0, and 4.5 μg/ml, respectively. TOFA at 1.0-20.0 μg/ml effectively blocked fatty acid synthesis and induced cell death in a dose-dependent manner[2]. TOFA was also cytotoxic to COC1 and COC1/DDP cells with IC50s of ~26.1 and 11.6 µg/ml, respectively. It inhibited the proliferation of the cancer cells examined in a time and dose dependent manner, arrested the cells in the G0/G1 cell cycle phase and induced apoptosis. In a human ovarian cancer mouse xenograft model, tumor growth rate was significantly inhibited by TOFA compared with the DMSO-treated control mice (1649 ± 356.3 vs. 5128 ± 390.4 mm3)[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.08mL 0.62mL 0.31mL |
15.41mL 3.08mL 1.54mL |
30.82mL 6.16mL 3.08mL |
参考文献 |
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