TVB-3166 |
Katalog-Nr.GC38710
One-Click Copy Product Info
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TVB-3166 ist ein oral verfÜgbarer, reversibler und selektiver Inhibitor der FettsÄuresynthase (FASN) mit IC50-Werten von 42 nM bzw. 81 nM fÜr die biochemische FASN- bzw. zellulÄre Palmitatsynthese. TVB-3166 induziert Apoptose und hemmt in-vivo-Xenotransplantat-Tumorwachstum.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1533438-83-3
Sample solution is provided at 25 µL, 10mM.
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TVB-3166 is an orally active fatty acid synthase (FASN) inhibitor (IC50=42nM). TVB-3166 inhibits cellular palmitate synthesis (IC50=81nM). TVB-3166 suppresses de novo palmitate synthesis and disrupts lipid raft structure. TVB-3166 downregulates PI3K/AKT/mTOR and β-catenin signaling and reduces c-Myc expression to inhibit tumor cell proliferation and survival. TVB-3166 inhibits SARS-CoV-2 spike protein S-acylation to reduce viral entry and spread. TVB-3166 can be used in research on lung cancer, ovarian cancer, prostate cancer, and other tumors, as well as COVID-19 and respiratory virus infections[1-4].
In vitro, SCC-9 ZsG and LN-1A cells were treated with 10-100µM TVB-3166 for 48 hours. TVB-3166 reduced cell viability, inhibited proliferation, promoted G0/G1 cell cycle arrest and apoptosis, and increased myogel adhesion[5]. PANC-1 and MIA PaCa-2 cells were treated with TVB-3166 for 48 hours. TVB-3166 increased the NADPH/NADP+ ratio and reactive oxygen species levels, promoted cytochrome c release and phosphatidylserine externalization and apoptosis, upregulated BIM, PUMA, and NOXA, and increased the proportion of apoptotic cells[6]. MOLM13, MV411, and Baf3-FLT3-ITD cells were treated with 100-250nM TVB-3166 for 1-5 days. TVB-3166 reduced pS6 levels, downregulated Gli1 expression, and decreased cell survival[7].
In vivo, BALB/c mice with respiratory syncytial virus (RSV) lung infection received 50mg/kg TVB-3166 via gavage twice daily for 3 days. TVB-3166 reduced lung RSV titers and decreased lung lymphocyte infiltration[8]. BALB-c-nude mice with PANC-1 xenografts received 100mg/kg TVB-3166 via gavage once daily for 18 days. TVB-3166 inhibited tumor growth[9]. SCID mice with tamoxifen-resistant MCF7/TamR cells implanted in the mammary fat pad received 60mg/kg TVB-3166 orally once daily for 8 weeks. TVB-3166 inhibited tamoxifen-resistant breast tumor growth[10].
References:[1] Yang Y, Zhang E, Mao X, et al. Targeting palmitoylation: A novel frontier in cancer biology and immunotherapy. Biochim Biophys Acta Rev Cancer. 2026 Feb;1881(1):189509.
[2] Montesdeoca N, López M, Ariza X, et al. Inhibitors of lipogenic enzymes as a potential therapy against cancer. FASEB J. 2020 Sep;34(9):11355-11381.
[3] Harris AL. Development of cancer metabolism as a therapeutic target: new pathways, patient studies, stratification and combination therapy. Br J Cancer. 2020 Jan;122(1):1-3.
[4] Bizeli ALV, Aquino IG, Cuadra-Zelaya FJM, et al. Isolation and Characterization of Putative Cancer Stem Cells from Oral Squamous Cell Carcinoma Cells. Anticancer Res. 2025 Nov;45(11):4803-4815.
[5] Aquino IG, Bastos DC, Cuadra-Zelaya FJM, et al. Anticancer properties of the fatty acid synthase inhibitor TVB-3166 on oral squamous cell carcinoma cell lines. Arch Oral Biol. 2020;113:104707.
[6] Vander Steen T, Espinoza I, Duran C, et al. Fatty acid synthase(FASN) inhibition cooperates with BH3 mimetic drugs to overcome resistance to mitochondrial apoptosis in pancreatic cancer. Neoplasia. 2025;62:101143.
[7] Kebenko M, Zhuang R, Hoffer K, et al. Downregulation of S6 Kinase and Hedgehog-Gli1 by Inhibition of Fatty Acid Synthase in AML with FLT3-ITD Mutation. Int J Mol Sci. 2025 Jun 14;26(12):5721.
[8] Ohol Y, Wang Z, Kemble G, et al. Direct Inhibition of Cellular Fatty Acid Synthase Impairs Replication of Respiratory Syncytial Virus and Other Respiratory Viruses. PLoS ONE. 2015 Dec 11;10(12):e0144648.
[9] Ventura R, Mordec K, Waszczuk J, et al. Inhibition of de novo palmitate synthesis by fatty acid synthase induces apoptosis in tumor cells by remodeling cell membranes, inhibiting signaling pathways, and reprogramming gene expression. EBioMedicine. 2015 Jul 2;2(7):808-24.
[10] Gruslova A, McClellan B, Balinda HU, et al. FASN inhibition as a potential treatment for endocrine-resistant breast cancer. Breast Cancer Res Treat. 2021;187(2):375-386.
| Cell experiment [1]: | |
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Cell lines |
SCC-9 ZsG cells (human oral squamous cell carcinoma cell line) and LN-1A cells (metastatic derivative of SCC-9 ZsG) |
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Preparation Method |
SCC-9 ZsG and LN-1A cells were maintained in DMEM/F-12 supplemented with 2% or 10% FBS at 37°C, 5% CO2. Cells were treated with TVB-3166 at 10-100µM for 48h for viability, proliferation, death, cell cycle, migration, adhesion and western blot analyses. |
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Reaction Conditions |
10-100µM; 48h |
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Applications |
TVB-3166 reduced cell viability and proliferation, promoted G0/G1 cell cycle arrest and Annexin V-PE positive cell death, increased adhesion to myogel, reduced SCC-9 ZsG migration, and decreased p-Akt level while increasing E-cadherin level in both cell lines. |
| Animal experiment [2]: | |
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Animal models |
Female BALB-c-nude mice |
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Preparation Method |
Mice were inoculated subcutaneously with PANC-1 or OVCAR-8 tumor cells or implanted with patient-derived tumor fragments, and when tumor size reached about 100-300 mm3, TVB-3166 was administered by oral gavage once daily (PANC-1: 30 or 100mg/kg for 18 days; OVCAR-8: 30/60/100mg/kg for 21 days) tumor size was measured twice weekly and tumors/plasma collected at study end for Western blot, pharmacokinetics and growth analysis. |
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Dosage form |
30/60/100mg/kg; p.o.; once daily for 18-21 days |
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Applications |
TVB-3166 inhibited PANC-1, OVCAR-8 xenograft tumor growth, reduced tumor pAkt(S473) in PANC-1 tumors, increased FASN protein expression in PANC-1 tumors, and caused body weight changes similar to vehicle-treated mice. |
| References: [1] Aquino IG, Bastos DC, Cuadra-Zelaya FJM, et al. Anticancer properties of the fatty acid synthase inhibitor TVB-3166 on oral squamous cell carcinoma cell lines. Arch Oral Biol. 2020 May;113:104707. [2] Ventura R, Mordec K, Waszczuk J, et al. Inhibition of de novo palmitate synthesis by fatty acid synthase induces apoptosis in tumor cells by remodeling cell membranes, inhibiting signaling pathways, and reprogramming gene expression. EBioMedicine. 2015 Jul 2;2(7):808-24. | |
| Cas No. | 1533438-83-3 | SDF | |
| Canonical SMILES | N#CC1=CC=C(C2CN(C(C3=CC(C4=NNC(C)=C4C)=C(C)C=C3C)=O)C2)C=C1. | ||
| Formula | C24H24N4O | M.Wt | 384.47 |
| Löslichkeit | DMSO: 62.5 mg/mL (162.56 mM) | Storage | Store at -20°C |
| 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 | 2.601 mL | 13.0049 mL | 26.0098 mL |
| 5 mM | 520.2 μL | 2.601 mL | 5.202 mL |
| 10 mM | 260.1 μL | 1.3005 mL | 2.601 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)