|5-(十四氧基)呋喃-2-甲酸|CsnPharm

CAS No.: 54857-86-2

TOFA Catalog No. CSN22083

Synonyms: RMI14514;MDL14514;5-(Tetradecyloxy)-2-furoic Acid

TOFA is a potent, reversible and competitive acetyl-CoA carboxylase (ACC) inhibitor which can inhibit fatty acid synthesis.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03755466	Rheumatoid Arthritis	Phase 2	Recruiting	November 20, 2023	Japan ... more >> Yukio Nakamura Recruiting Matsumoto, Nagano, Japan, 3908621 Contact: Yukio Nakamura, MD, PhD +81-263-37-2659 yxn14@aol.jp Principal Investigator: Yukio Nakamura, MD, PhD Collapse <<
NCT03288324	Cutaneous Lupus ... more >> Systemic Lupus Erythematosus Collapse <<	Phase 1 Phase 2	Recruiting	August 2020	United States, Ohio ... more >> Cincinnati Childrens Hospital Medical Center Recruiting Cincinnati, Ohio, United States, 45229 Contact: Angela SR CRC 513-803-2118 angela.merritt@cchmc.org Collapse <<
NCT01741493	Rheumatoid Arthritis	Phase 1	Completed	-	United States, Florida ... more >> Site Reference ID/Investigator# 95817 Miami, Florida, United States, 33136 United States, Ohio Site Reference ID/Investigator# 95816 Cincinnati, Ohio, United States, 45255 United States, Pennsylvania Site Reference ID/Investigator# 95815 Duncansville, Pennsylvania, United States, 16635 United States, Texas Site Reference ID/Investigator# 92153 Austin, Texas, United States, 78744 United States, Utah Site Reference ID/Investigator# 97177 Orem, Utah, United States, 84058 Collapse <<

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参考文献

[2] 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
[3] Li S, et al. TOFA suppresses ovarian cancer cell growth in vitro and in vivo. Mol Med Rep. 2013 Aug;8(2):373-8

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0820 mL
- 15.4102 mL
- 30.8204 mL
- 5 mM
- 0.6164 mL
- 3.0820 mL
- 6.1641 mL
- 10 mM
- 0.3082 mL
- 1.5410 mL
- 3.0820 mL

技术信息

CAS号

54857-86-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H32O4

运输

蓝冰

分子量

324.45

别名

RMI14514;MDL14514;5-(Tetradecyloxy)-2-furoic Acid

溶解度

DMSO	64.0 mg/mL (197.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03755466	Rheumatoid Arthritis	Phase 2	Recruiting	November 20, 2023	Japan ... more >> Yukio Nakamura Recruiting Matsumoto, Nagano, Japan, 3908621 Contact: Yukio Nakamura, MD, PhD +81-263-37-2659 yxn14@aol.jp Principal Investigator: Yukio Nakamura, MD, PhD Collapse <<
NCT03288324	Cutaneous Lupus ... more >> Systemic Lupus Erythematosus Collapse <<	Phase 1 Phase 2	Recruiting	August 2020	United States, Ohio ... more >> Cincinnati Childrens Hospital Medical Center Recruiting Cincinnati, Ohio, United States, 45229 Contact: Angela SR CRC 513-803-2118 angela.merritt@cchmc.org Collapse <<
NCT01741493	Rheumatoid Arthritis	Phase 1	Completed	-	United States, Florida ... more >> Site Reference ID/Investigator# 95817 Miami, Florida, United States, 33136 United States, Ohio Site Reference ID/Investigator# 95816 Cincinnati, Ohio, United States, 45255 United States, Pennsylvania Site Reference ID/Investigator# 95815 Duncansville, Pennsylvania, United States, 16635 United States, Texas Site Reference ID/Investigator# 92153 Austin, Texas, United States, 78744 United States, Utah Site Reference ID/Investigator# 97177 Orem, Utah, United States, 84058 Collapse <<
NCT03274076	Systemic Sclerosis ... more >> Scleroderma Collapse <<	Phase 1 Phase 2	Active, not recruiting	December 2019	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48104 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15261 Collapse <<

TOFA Catalog No. CSN22083

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