1. Metabolic Enzyme/Protease
  2. Fatty Acid Synthase (FAS)
  3. TVB-3664

TVB-3664 

Cat. No.: HY-120062
Handling Instructions

TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.

For research use only. We do not sell to patients.

TVB-3664 Chemical Structure

TVB-3664 Chemical Structure

CAS No. : 2097262-58-1

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Description

TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression[1][2].

IC50 & Target

FASN[1][2].

In Vitro

TVB-3664 (0-1 μM, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines[1].
TVB-3664 decreases viability in multiple tumor cell lines from solid and hematopoietic tumor types[1].

Cell Proliferation Assay[1]

Cell Line: CaCo2, HT29 and LIM2405 cell lines.
Concentration: 0-1 μM.
Incubation Time: 7 days.
Result: Showed anti-tumor activity.
In Vivo

TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively[1].

Animal Model: Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis[1].
Dosage: 3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).
Administration: Oral gavage daily for 4 weeks.
Result: Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

468.47

Formula

C₂₅H₂₃F₃N₄O₂

CAS No.

2097262-58-1

SMILES

CC1=C(C=C(C(C)=C1)C(N2CC(C2)C3=CC=C(C=C3)C#N)=O)C4=C(N=C(N4)C(F)(F)F)COC

Shipping

Room temperature in continental US; may vary elsewhere

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TVB-3664
Cat. No.:
HY-120062
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TVB-3664

Cat. No.: HY-120062