Art. -Nr.: HY-120394

TVB-3166

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC₅₀s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.

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Reinheit: 99.69%
CAS. Nr.: 1533438-83-3
Formel: C₂₄H₂₄N₄O
Molecular Weight:384.47

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TVB-3166 Chemical Structure

CAS. Nr.: 1533438-83-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)^[1]

In Vitro

ISX-9 promotes neurogenesis in vivo, enhancing the proliferation and differentiation of hippocampal subgranular zone (SGZ) neuroblasts, and the dendritic arborization of adult-generated dentate gyrus neurons. At 2.5-20 μM, ISX-9 has been shown to dose-dependently trigger neurogenesis and block gliogenesis in adult rat hippocampal stem cells through a calcium-activated signaling pathway dependent on myocyte-enhancer factor 2-dependent gene expression^[1].
Molecular exploration of ISX-9-induced regulation of neurogenesis (via FACS and microarray of SGZ stem and progenitor cells) suggested the involvement of the myocyte-enhancer family of proteins (Mef2)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

CALU-6 tumor cells
Concentration:

0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

24 hours
Result:

Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC₅₀ value of 0.10 μM.

Cell Viability Assay^[1]

Cell Line:

90 different tumor cell lines (such as CALU-6 NSCLC cell line, NCI-H1975 NSCLC cell line)
Concentration:

0.02 or 0.20 μM
Incubation Time:

7 days
Result:

Dose-dependent induction of cell death was observed in all tumor cell lines.

Western Blot Analysis^[1]

Cell Line:

COLO-205 and A549 cells
Concentration:

0.2 μM
Incubation Time:

48 hours
Result:

Inhibited β-catenin pathway signal transduction and transcriptional activity.

In Vivo

TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth^[1].
TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB-c-nude mice^[1]
Dosage:

30, 60, or 100 mg/kg
Administration:

Oral gavage; once daily
Result:

Inhibited xenograft tumor growth.

Animal Model:

Female BALB-c-nude mice^[1]
Dosage:

30, 60, or 100 mg/kg (Pharmacokinetic Study)
Administration:

Oral gavage; once daily
Result:

The concentration was approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively.

Chemical Information

CAS. Nr. 1533438-83-3
Appearance Solid
Molecular Weight 384.47
Formel C₂₄H₂₄N₄O
Color White to off-white
SMILES

N#CC1=CC=C(C2CN(C(C3=CC(C4=NNC(C)=C4C)=C(C)C=C3C)=O)C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All ELISAIHCWBCell Proliferation/Viability AssayIn Vivo Efficacy Study2D/3D Cell Culture and Differentiation

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Journal Impact Factor

Nat Metab

Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication. [Abstract]

2021 Nov;3(11):1466-1475. PMID: 34580494
Nat Commun

Lipogenic enzyme FASN promotes mutant p53 accumulation and gain-of-function through palmitoylation. [Abstract]

2025 Feb 19;16(1):1762. PMID: 39971971

TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]

Inhibition of FASN by TVB-3166 reduced the protein levels of mutp53, but not wtp53, in different cells. Cells were treated with the small-molecule FASN inhibitor TVB-3166 (TVB) at the indicated concentrations for 24 h and subjected to Western blot analysis.

TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]

The FASN inhibitor TVB-3166 (TVB, 72 h) displayed a more pronounced inhibitory effect on AIG in cancer cells carrying mutp53 compared with cells with mutp53 KO (a) or knockdown (b). Left in a: Representative images. Scale bar: 200 μm.

TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]

TVB-3166 (TVB) displayed a more pronounced inhibitory effect on the growth of orthotopic tumors formed by SK-BR3 (R175H) cells than tumors formed by SK-BR3 with mutp53 KO. Mice were treated with TVB-3166 (60 mg/kg; i.g.) once every two days for 3 weeks when tumor sizes reached ~30 mm³.

TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]

TVB-3166 (40 μM) treatment displayed a more pronounced inhibitory effect on human colorectal tumor organoids expressing mutp53 compared with organoids expressing wtp53. Left panels: Representative images of different organoids expressing mutp53 or wtp53, which were treated with or without TVB-3166 for 48 h. Scale bar: 50 μm. Right panel: The relative viability of mutp53 and wtp53 organoids.
J Immunother Cancer

Targeting B7-H3 inhibition-induced activation of fatty acid synthesis boosts anti-B7-H3 immunotherapy in triple-negative breast cancer. [Abstract]

2025 Apr 12;13(4):e010924. PMID: 40221152
J Transl Med

Metabolic reprogramming based on RNA sequencing of gemcitabine-resistant cells reveals the FASN gene as a therapeutic for bladder cancer. [Abstract]

2024 Jan 13;22(1):55. PMID: 38218866
Br J Cancer

Transcriptome analysis of newly established carboplatin-resistant ovarian cancer cell model reveals genes shared by drug resistance and drug-induced EMT. [Abstract]

2023 Mar;128(7):1344-1359. PMID: 36717670
Neurosci Bull

Targeting Phospholipid Metabolism as an Effective Hearing Protection Strategy. [Abstract]

2025 Jun 28. PMID: 40580390
EMBO Rep

Exogenous L-Alanine promotes phagocytosis of multidrug-resistant bacterial pathogens. [Abstract]

2023 Dec 6;24(12):e49561. PMID: 37943703
ACS Omega

Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]

2024 Feb 28;9(10):11870-11882. PMID: 38496939
J Cell Sci

Tumor acidosis supports cancer cell lipid uptake via a rapid transporter-independent mechanism. [Abstract]

2025 Apr 7:jcs.263688. PMID: 40190115
Biomed Pharmacother

Modeling of glucocorticoid resistance in multiple myeloma reveals mechanisms and markers of glucocorticoid resistance. [Abstract]

2025 Oct 24:192:118656. PMID: 41138658

TVB-3166 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Oct 24:192:118656. [Abstract]

Enzyme-linked immunosorbent assay (ELISA) was used to determine the FASN content of xenograft tumors in each group. The ELISA results showed that TVB-3166 (60 mg/kg; i.g.; 5 weeks) reduced the FASN gene of the tumor.

TVB-3166 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Oct 24:192:118656. [Abstract]

Statistical analysis was performed on the rate of KI67- and TUNEL-positive cells in each group of xenograft tumors by immunohistochemical staining (IHC). The corrected total cell fluorescence (CTCF) of BODIPY staining was used to quantitatively detect the lipid content of xenograft tumors in each group. The results showed that TVB-3166 (60 mg/kg; i.g.; 5 weeks) treatment can reduce lipid accumulation, inhibit cell proliferation and increase the apoptosis rate.
University of Rijeka

2023.
McGill University

2021 Aug, 30347448.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6010 mL

13.0049 mL

26.0098 mL

5 mM

0.5202 mL

2.6010 mL

5.2020 mL

10 mM

0.2601 mL

1.3005 mL

2.6010 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ventura R, 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(8):808-24. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6010 mL	13.0049 mL	26.0098 mL	65.0246 mL
	5 mM	0.5202 mL	2.6010 mL	5.2020 mL	13.0049 mL
	10 mM	0.2601 mL	1.3005 mL	2.6010 mL	6.5025 mL
	15 mM	0.1734 mL	0.8670 mL	1.7340 mL	4.3350 mL
	20 mM	0.1300 mL	0.6502 mL	1.3005 mL	3.2512 mL
	25 mM	0.1040 mL	0.5202 mL	1.0404 mL	2.6010 mL
	30 mM	0.0867 mL	0.4335 mL	0.8670 mL	2.1675 mL
	40 mM	0.0650 mL	0.3251 mL	0.6502 mL	1.6256 mL
	50 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3005 mL
	60 mM	0.0433 mL	0.2167 mL	0.4335 mL	1.0837 mL
	80 mM	0.0325 mL	0.1626 mL	0.3251 mL	0.8128 mL
	100 mM	0.0260 mL	0.1300 mL	0.2601 mL	0.6502 mL

Keywords

TVB-3166

12 Cited Publications

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TVB-3166

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TVB-3166

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TVB-3166

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TVB-3166

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TVB-3166 Related Classifications

HY-120394 Related Classifications