TVB-3664

Catalog No.S8563 Batch:S856301

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Technical Data

Formula

C25H23F3N4O2
Molecular Weight 468.47 CAS No. 2097262-58-1
Solubility (25°C)* In vitro DMSO 94 mg/mL (200.65 mM)
Ethanol 50 mg/mL (106.73 mM)
Water Insoluble
* <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.)

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Biological Activity

Description TVB-3664 is a potent, selective, orally active and reversible inhibitor of fatty acid synthase (FASN) with IC50 of 0.018 μM and 0.012 μM for human and mouse cell palmitate synthesis, respectively.
Targets
FASN [1]
(mouse cell palmitate synthesis)		 FASN [1]
(human cell palmitate synthesis)
0.012 μM 0.018 μM
In vitro

TVB-3664 induces FASN inhibition with significantly reduced tubulin palmitoylation and mRNA expression. Disrupted microtubule organization in tumor cells is an additional consequence of FASN inhibition. TVB-3664 combined with taxane treatment enhances inhibition of in vitro tumor cell growth compared to treatmentwith either agent alone.[1]
In vivo

In lung, ovarian, prostate, and pancreatic tumor xenograft studies, TVB-3664 and paclitaxel or docetaxel combine to inhibit xenograft tumor growth with significantly enhanced anti-tumor activity. Tumor regression is observed in 3 of 6 tumor xenograftmodels.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Calu-6 cells, A549 cells

  • Concentrations

    50 nM

  • Incubation Time

    48 h, 72 h

  • Method

    Calu-6 cells are treated with 50 nM TVB-3664 for 48 h. Paclitaxel is added to the cell culture media to a final concentration of 6 nM. After the 2 h of incubation with paclitaxel, cells and supernatant are collected for analysis.
Animal Study:

[1]
  • Animal Models

    female BALB-c-nude mice

  • Dosages

    10 mg/kg, 2.5 mg/kg

  • Administration

    PO, IV

Selleck's TVB-3664 has been cited by 5 publications

De novo lipogenesis fuels adipocyte autophagosome and lysosome membrane dynamics [ Nat Commun, 2023, 14(1):1362] PubMed: 36914626
Dual targeting of hepatocyte DGAT2 and stellate cell FASN alleviates nonalcoholic steatohepatitis in mice [ bioRxiv, 2023, 2023.07.05.547848] PubMed: 37461560
ATP citrate lyase controls hematopoietic stem cell fate and supports bone marrow regeneration [ EMBO J, 2022, e109463] PubMed: 35229328
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] PubMed: 34580494
Metabolomic credentialing of murine carcinogen-induced urothelial cancer [ Sci Rep, 2021, 11(1):22085] PubMed: 34764423

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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.