TVB-3166

TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.

TVB-3166 Chemical Structure

TVB-3166 Chemical Structure

CAS No. 1533438-83-3

Purity & Quality Control

TVB-3166 Related Products

Biological Activity

Description TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
Targets
FASN [1]
(Cell-free assay)
0.042 μM
In vitro
In vitro

TVB-3166, a FAS inhibitor, assesses its ability to inhibit SARS-CoV-2-mNG infection with an EC50 of 11 nM.[2]

Cell Research Cell lines HEK293T-hACE2, Caco-2 and MEF-hACE2 cells
Concentrations 320 nM
Incubation Time 16 h
Method

HEK293T-hACE2 (1 × 105 cells per well), Caco-2 (2 × 105 cells per well) or MEF-hACE2 cells (5 × 104 cells per well) were seeded in 24-well plates in culture medium and incubated at 37 °C, 5% CO2 cell culture incubator. Inhibitor dose titration is a fourfold serial dilution of selected eight inhibitors with different starting concentrations of 20 µM (orlistat, FASN-IN-4, FT113), 320 nM (TVB-2640, TVB-3166, GSK-214069) or 80 nM (TVB-3664, remdesivir). Diluted inhibitors were added to the cells 16 h before infection and maintained in the medium during infection. After being transferred to the BSL3 facility, pre-treated cells were infected with the SARS-CoV-2-mNG virus (icSARS-CoV-2-mNG) with an MOI of 0.01. Fluorescence assay and quantification of SARS-CoV-2 infection were performed at 24 h after infection.

Chemical Information & Solubility

Molecular Weight 384.47 Formula

C24H24N4O

CAS No. 1533438-83-3 SDF --
Smiles CC1=C(C)C(=N[NH]1)C2=C(C)C=C(C)C(=C2)C(=O)N3CC(C3)C4=CC=C(C=C4)C#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 77 mg/mL ( (200.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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