TVB-3664

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.

TVB-3664 Chemical Structure

TVB-3664 Chemical Structure

CAS No. 2097262-58-1

Purity & Quality Control

Batch: S856301 DMSO]94 mg/mL]false]Ethanol]50 mg/mL]false]Water]Insoluble]false Purity: 99.69%
99.69

TVB-3664 Related Products

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
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]

Cell Research 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. After the 2 h of incubation, cells and supernatant are collected for analysis.

In Vivo
In vivo

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

Animal Research Animal Models female BALB-c-nude mice
Dosages 10 mg/kg, 2.5 mg/kg
Administration PO, IV

Chemical Information & Solubility

Molecular Weight 468.47 Formula

C25H23F3N4O2

CAS No. 2097262-58-1 SDF --
Smiles CC1=CC(=C(C=C1C2=C(NC(=N2)C(F)(F)F)COC)C(=O)N3CC(C3)C4=CC=C(C=C4)C#N)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 94 mg/mL ( (200.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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