TVB-3166

Catalog No.S3576 Batch:S357602

Technical Data

Formula

C₂₄H₂₄N₄O

Molecular Weight

384.47

CAS No.

1533438-83-3

Solubility (25°C)*

In vitro

DMSO

77 mg/mL (200.27 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.64mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 12.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.85mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

Protocol (from reference)

Cell Assay:^{^[2]}	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.

Cell Assay:^{^[2]}

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.

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.