TVB-3664 |
Catalog No.GC19976
One-Click Copy Product Info
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TVB-3664 is an orally active fatty acid synthase (FASN) inhibitor with IC50 values of 18 nM and 12 nM for human and mouse FASN, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097262-58-1
Sample solution is provided at 25 µL, 10mM.
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TVB-3664 is an orally active fatty acid synthase (FASN) inhibitor with IC50 values of 18 nM and 12 nM for human and mouse FASN, respectively[1]. TVB-3664 is an analog of TVB-3166 and has shown antitumor activity in preclinical studies in breast cancer, prostate, colorectal, and lung[2]. TVB-3664 strongly inhibits the SARS-CoV-2 virus with an EC50 value of 0.07 nM, which is five times more potent than remdesivir (EC50 = 0.4 nM)[3].
In vitro, treatment of A549 lung cancer cells with TVB-3664 (50 nM) for 72 h resulted in 67% and 92% loss of palmitoyl-α-tubulin and palmitoyl-β-tubulin, respectively[1]. TVB-3664 (200 nM) treatment of multiple colorectal cancer (CRC) cell lines significantly reduced the fatty acid and phospholipid content of the cells, and inhibited the proliferation and survival of tumor cells by reducing the activity of the Akt and Erk1/2 pathways [4].
In vivo, TVB-3664 (6 mg/kg) was orally treated with mice with colorectal cancer for 4 weeks, which reduced the expression of sphingosine kinase 2 (SPHK2) in tumor cells and activated the focal adhesion markers p-FAK and p-paxillin protein [5]. TVB-3664 (0.3-10 mg/kg) was orally treated with mice with fatty liver disease for 8 weeks, which dose-dependently reduced the liver histological severity score and the level of the pro-inflammatory cytokine IL-1β [6].
References:
[1] Heuer T S, Ventura R, Mordec K, et al. FASN inhibition and taxane treatment combine to enhance anti-tumor efficacy in diverse xenograft tumor models through disruption of tubulin palmitoylation and microtubule organization and FASN inhibition-mediated effects on oncogenic signaling and gene expression[J]. EBioMedicine, 2017, 16: 51-62.
[2] Aquino I G, Bastos D C, Cuadra-Zelaya F J M, et al. Anticancer properties of the fatty acid synthase inhibitor TVB-3166 on oral squamous cell carcinoma cell lines[J]. Archives of oral biology, 2020, 113: 104707.
[3] Chu J, Xing C, Du Y, et al. Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication[J]. Nature metabolism, 2021, 3(11): 1466-1475.
[4]Zaytseva Y Y, Rychahou P G, Le A T, et al. Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derived xenograft model of colorectal cancer[J]. Oncotarget, 2018, 9(37): 24787.
[5]Jafari N, Drury J, Morris A J, et al. De novo fatty acid synthesis-driven sphingolipid metabolism promotes metastatic potential of colorectal cancer[J]. Molecular Cancer Research, 2019, 17(1): 140-152.
[6]O’Farrell M, Duke G, Crowley R, et al. FASN inhibition targets multiple drivers of NASH by reducing steatosis, inflammation and fibrosis in preclinical models[J]. Scientific Reports, 2022, 12(1): 15661.
Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation method | A549 cells was treated for 16 or 72 h with 20 μM 2-bromopalmitate or 50 nM TVB-3664. |
Reaction Conditions | 50 nM ; 16 or 72 h |
Applications | A549 cells treated with 50 nM TVB-3664 for 72 h showed a 67% and 92% loss of palmitoyl-α-tubulin and palmitoyl-β-tubulin, respectively. |
Animal experiment [2]: | |
Animal models | NSG mice |
Preparation method | Mice were given a vehicle (30% PEG400) or 6 mg/kg of TVB-3664 by oral gavage daily for 4 weeks. Tissues were lysed and Western blot was performed. |
Dosage form | 6mg/kg; p.o. |
Applications | TVB-3664 treatment leads to significant reduction of SPHK2 expression and activation of p-FAK and p-paxillin. |
References: [1]Heuer T S, Ventura R, Mordec K, et al. FASN inhibition and taxane treatment combine to enhance anti-tumor efficacy in diverse xenograft tumor models through disruption of tubulin palmitoylation and microtubule organization and FASN inhibition-mediated effects on oncogenic signaling and gene expression[J]. EBioMedicine, 2017, 16: 51-62. [2]Jafari N, Drury J, Morris A J, et al. De novo fatty acid synthesis-driven sphingolipid metabolism promotes metastatic potential of colorectal cancer[J]. Molecular Cancer Research, 2019, 17(1): 140-152. | |
| Cas No. | 2097262-58-1 | SDF | |
| Formula | C25H23F3N4O2 | M.Wt | 468.47 |
| Solubility | DMSO : 10 mg/mL (21.35 mM; Need ultrasonic) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1346 mL | 10.673 mL | 21.3461 mL |
| 5 mM | 426.9 μL | 2.1346 mL | 4.2692 mL |
| 10 mM | 213.5 μL | 1.0673 mL | 2.1346 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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)