5-(十四烷基氧)-2-糠酸

应用生物活性靶点体外研究体内研究 5-(十四烷基氧)-2-糠酸试剂级价格

5-(十四烷基氧)-2-糠酸

CAS号:54857-86-2
英文名:5-(TETRADECYLOXY)-2-FUROIC ACID
中文名:5-(十四烷基氧)-2-糠酸
CBNumber:CB4759746
分子式:C19H32O4
分子量:324.45
MOL File:54857-86-2.mol

5-(十四烷基氧)-2-糠酸化学性质

熔点 :112-115 °C
沸点 :441.7±25.0 °C(Predicted)
密度 :1.003±0.06 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :DMSO: 2.5 mg/mL
形态 :solid
酸度系数(pKa) :3.55±0.10(Predicted)
颜色 :white to beige
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

安全信息

WGK Germany :2
RTECS号 :LU0288000
海关编码 :29321900

5-(十四烷基氧)-2-糠酸性质、用途与生产工艺

应用 5-(十四烷基氧)-2-糠酸可作为有机合成中间体和医药中间体，可用于实验室研发过程和化工医药生产过程中。
生物活性 TOFA (5-(Tetradecyloxy)-2-furoic acid, Tyrphostin 46,Tyrphostin A46,Tyrphostin B40)是acetyl-CoA carboxylase-α (ACCA)的变构抑制剂。在细胞内TOFA转化为TOFyl-CoA (5-tetradecyloxy-2-furoyl-CoA)，对ACCA具有变构抑制作用。 TOFA阻止脂肪酸合成，并以剂量依赖性方式诱导细胞死亡。
靶点
Target Value
ACCA
()
体外研究

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 IC ₅₀ 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. TOFA is found to be cytotoxic to COC1 and COC1/DDP cells with IC ₅₀ 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. 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.
体内研究

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 mm ³ . 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.