Denifanstat (TVB-2640)

Catalog No.S9714 Batch:S971402

Technical Data

Formula

C₂₇H₂₉N₅O

Molecular Weight

439.55

CAS No.

1399177-37-7

Solubility (25°C)*

In vitro

DMSO

88 mg/mL (200.2 mM)

Ethanol

88 mg/mL (200.2 mM)

Water

Insoluble

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

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

4.4mg/ml

Taking the 1 mL working solution as an example, add 50 μL 88 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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

Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.

Targets

FAS ^[1]

In vitro

TVB-2640 markedly inhibits SARS-CoV-2 with EC50s of 4 nM. TVB-2640 could strikingly inhibit SARS-CoV-2 new variants with similar inhibitory effects on the early-lineage SARS-CoV-2 (USA-WA1/2020) virus.^[2]

In vivo

TVB-2640 shows significant in vivo antiviral activity and protects SARS-CoV-2-infected mice for survival.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines HEK293T-hACE2, Caco-2, MEF-hACE2 cells Concentrations 100 nM for HEK293T-hACE2 cells; 2 µM for NCI-H1355, NCI-1437 and Caco-2 cells; 1 µM for MEF-hACE2 cells Incubation Time 16+24 h Method Indicated cells were pre-treated with TVB-2640 from 16 h before infection and then infected with SARS-CoV-2-mNG. Fluorescence images were acquired at 48 hpi. Hoechst 33342 was used for nuclear staining. Assessment of anti-SARS-CoV-2 ability of FAS inhibitors in multiple cell lines. Indicated cells were pre-treated with TVB-2640 and infected with SARS-CoV-2 for 24 h, after infection cells were collected for quantification of intracellular viral RNA by qPCR. (Data sourced from selleck products)
Animal Study:^{^[2]}	Animal Models K18-hACE2 transgenic mice infected by SARS-CoV-2 Dosages 8 mg kg-1 body weight Administration i.p. (Data sourced from selleck products)

Cell Assay:^{^[2]}

Cell lines
HEK293T-hACE2, Caco-2, MEF-hACE2 cells
Concentrations
100 nM for HEK293T-hACE2 cells; 2 µM for NCI-H1355, NCI-1437 and Caco-2 cells; 1 µM for MEF-hACE2 cells
Incubation Time
16+24 h
Method
Indicated cells were pre-treated with TVB-2640 from 16 h before infection and then infected with SARS-CoV-2-mNG. Fluorescence images were acquired at 48 hpi. Hoechst 33342 was used for nuclear staining. Assessment of anti-SARS-CoV-2 ability of FAS inhibitors in multiple cell lines. Indicated cells were pre-treated with TVB-2640 and infected with SARS-CoV-2 for 24 h, after infection cells were collected for quantification of intracellular viral RNA by qPCR.

(Data sourced from selleck products)

Animal Study:^{^[2]}

Animal Models
K18-hACE2 transgenic mice infected by SARS-CoV-2
Dosages
8 mg kg-1 body weight
Administration
i.p.

(Data sourced from selleck products)

References

Selleck's Denifanstat (TVB-2640) has been cited by 8 publications

Organismal metabolism regulates the expansion of oncogenic PIK3CA mutant clones in normal esophagus [ Nat Genet, 2024, 10.1038/s41588-024-01891-8]	PubMed: 39169259
Formate promotes invasion and metastasis in reliance on lipid metabolism [ Cell Rep, 2023, 42(9):113034]	PubMed: 37651228
FASN multi-omic characterization reveals metabolic heterogeneity in pancreatic and prostate adenocarcinoma [ J Transl Med, 2023, 21(1):32]	PubMed: 36650542
Imaging the metabolic reprograming of fatty acid synthesis pathway enables new diagnostic and therapeutic opportunity for breast cancer [ Cancer Cell Int, 2023, 23(1):83]	PubMed: 37120513
The Deubiquitinase USP13 Maintains Cancer Cell Stemness by Promoting FASN Stability in Small Cell Lung Cancer [ Front Oncol, 2022, 12:899987]	PubMed: 35898882
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4]	PubMed: 34580494
Metabolic convergence on lipogenesis in RAS, BCR-ABL, and MYC-driven lymphoid malignancies [ Cancer Metab, 2021, 9(1):31]	PubMed: 34399819
Molecular Response to PARP1 Inhibition in Ovarian Cancer Cells as Determined by Mass Spectrometry Based Proteomics [ bioRxiv, 2021, 10.1101/2021.03.12.435005]	PubMed: None

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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.