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Tolrestat_Medchemexpress前沿研究进展

发布时间:2018/7/16 14:52:03 阅读人数:820

TOFA产品描述:TOFA (RMI14514;MDL14514)是乙酰辅酶A羧化酶-α (ACCA )的变构抑制剂。
TOFA产品描述:TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).In Vitro: TOFA (5-tetradecyloxy-2-furoic acid) is cytotoxic to lung cancer cells NCI-H460 and colon carcinoma cells HCT-8 and HCT-15, with an IC50 at approximately 5.0, 5.0, and 4.5 μg/mL, respectively. TOFA at 1.0–20.0 μg/mL effectively blocks fatty acid synthesis and induces cell death in a dose-dependent manner[1]. TOFA is found to be cytotoxic to COC1 and COC1/DDP cells with IC50 values of ~26.1 and 11.6 µg/mL, respectively. TOFA inhibits the proliferation of the cancer cells examined in a time and dose dependent manner, arrests the cells in the G0/G1 cell cycle phase and induces apoptosis[2]. Acetyl-CoA-carboxylase-α (ACCA) is a key enzyme in the regulation of fatty acids synthesis. Inhibition of ACCA by TOFA decreases fatty acid synthesis and induces caspase activation and cell death in most PCa cell lines[3].In Vivo: TOFA inhibits COC1/DDP cell growth in ovarian tumor mouse xenografts. The tumor growth rate is signifi¬cantly inhibited by TOFA compared with the DMSO treated control mice (1649±356.3 vs. 5128±390.4 mm3. No toxicity is observed in the heart, liver, spleen, lung, kidney and intestinal tissues. By inhibiting ACC, TOFA may be a promising small molecule agent for ovarian cancer therapy[2].

研究领域:Immunology/Inflammation

靶点:Salt-inducible Kinase (SIK)

相关产品:HG-9-91-01  |  

Alternative_Names:RMI14514;MDL14514

MWt:324.45

Formula:C19H32O4

SMILES:O=C(C1=CC=C(OCCCCCCCCCCCCCC)O1)O

Research_Area:Cancer



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