TOFA (RMI14514) (Synonyms: RMI 14514, 5(Tetradecyloxy)2furoic Acid) |
| رقم الكتالوجGC32715 |
TOFA (RMI14514) (RMI14514 ؛ MDL14514) هو مثبط خيفي من acetyl-CoA carboxylase-α ؛ (جمعية المحاسبين القانونيين المعتمدين).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 54857-86-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
TOFA (RMI14514) is a conformational inhibitor of acetyl-CoA carboxylase-α (ACCA). Within cells, TOFA is converted into TOFyl-CoA (5-tetradecyloxy-2-furoyl-CoA), which conformationally inhibits the rate-limiting enzyme ACCA in the fatty acid synthesis pathway[1]. TOFA prevents fatty acid synthesis and induces cancer cell death[2]. TOFA is a highly effective lipid-lowering agent[3].
In vitro, TOFA (0-50.0µg/ml) treatment of lung cancer cells (NCI-H460) and colon cancer cells (HCT-8 and HCT-15) for 72hours showed strong cytotoxicity, inducing apoptosis in a dose-dependent manner, with IC50 values of approximately 5.0µg/ml, 5.0µg/ml, and 4.5µg/ml, respectively[1]. Similarly, TOFA (0-50.0µg/ml) had IC50 values of approximately 26.1µg/mL for COC1 cells and 11.6µg/mL for COC1/DDP cells, blocking the cell cycle at the G0/G1 phase and inducing apoptosis[4]. TOFA (10µg/ml, 24h) treatment of PCa cell lines induced caspase activation and cell death[5]. TOFA (2-10 µg/ml) treatment of ACHN and 786-O cells for 48hours had IC50 values of approximately 6.06µg/ml and 5.36µg/ml, respectively[6].
In vivo, TOFA (50 mg/kg) administered intraperitoneally daily for two weeks in a xenograft mouse model of human ovarian cancer significantly inhibited tumor growth rate, with no toxicity observed in the heart, liver, spleen, lungs, kidneys, and intestinal tissues[4].
References:
[1] Wang C , Xu C , Sun M ,et al.Acetyl-CoA Carboxylase-α Inhibitor TOFA Induces Human Cancer Cell Apoptosis[J].Biochemical and Biophysical Research Communications, 2009, 385(3):302-306.
[2] Tan W , Zhong Z , Wang S ,et al.Berberine Regulated Lipid Metabolism in the Presence of C75, Compound C, and TOFA in Breast Cancer Cell Line MCF-7[J].Evidence-based complementary and alternative medicine: eCAM, 2015(10).
[3] Leyuan, ChenYuqing, DuanHuiqiang, et al. Acetyl-CoA carboxylase (ACC) as a therapeutic target for metabolic syndrome and recent developments in ACC1/2 inhibitors[J].Expert opinion on investigational drugs, 2019, 28(7a12).
[4] Li S, Qiu L, Wu B et al. TOFA suppresses ovarian cancer cell growth in vitro and in vivo. Mol Med Rep. 2013 Aug;8(2):373-8.
[5]Guseva NV, et al. TOFA (5-tetradecyl-oxy-2-furoic acid) reduces fatty acid synthesis, inhibits expression of AR, neuropilin-1 and Mcl-1 and kills prostate cancer cells independent of p53 status. Cancer Biol Ther. 2011 Jul 1;12(1):80-5.
[6]Dejiao H , Xuan S , Hongxia Y ,et al.TOFA induces cell cycle arrest and apoptosis in ACHN and 786-O cells through inhibiting PI3K/Akt/mTOR pathway[J].Journal of Cancer, 2018, 9(15):2734-2742.
|
Cell experiment [1]: |
|
|
Cell lines |
NCI-H460, HCT-8, HCT-15 cells |
|
Preparation method |
cells (5000/well) were seeded in 96-well plates overnight and then exposed to TOFA at 1.0-50.0μg/ml for 72 h. |
|
Reaction Conditions |
1.0-50.0μg/ml; 72 h |
|
Applications |
TOFA showed strong cytotoxicity to all three human cancer cell lines, with an IC50 at approximately 5.0, 5.0, and 4.5μg/ml for NCI-H460, HCT-8, and HCT-15 cells. |
|
Animal experiment [2]: |
|
|
Animal models |
Female athymic BALB/c nude mice |
|
Preparation method |
The cells were subcutaneously injected into both right and left flanks of each mouse. Twenty days later, mice treated with 50μl DMSO (control group) or treated with TOFA (50 mg/kg). The drugs were injected intraperitoneally daily for two weeks. |
|
Dosage form |
50 mg/kg; i.p. |
|
Applications |
The tumor growth rate was significantly inhibited by TOFA compared with the DMSO-treated control mice. |
|
References: [1] Wang C , Xu C , Sun M ,et al.Acetyl-CoA Carboxylase-α Inhibitor TOFA Induces Human Cancer Cell Apoptosis[J].Biochemical and Biophysical Research Communications, 2009, 385(3):302-306. [2] Li S, Qiu L, Wu B et al. TOFA suppresses ovarian cancer cell growth in vitro and in vivo. Mol Med Rep. 2013 Aug;8(2):373-8. |
|
| Cas No. | 54857-86-2 | SDF | |
| المرادفات | RMI 14514, 5(Tetradecyloxy)2furoic Acid | ||
| Canonical SMILES | O=C(C1=CC=C(OCCCCCCCCCCCCCC)O1)O | ||
| Formula | C19H32O4 | M.Wt | 324.45 |
| الذوبان | DMSO : ≥ 34 mg/mL (104.79 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0821 mL | 15.4107 mL | 30.8214 mL |
| 5 mM | 0.6164 mL | 3.0821 mL | 6.1643 mL |
| 10 mM | 0.3082 mL | 1.5411 mL | 3.0821 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *