Home Metabolism Fatty Acid Synthase inhibitor TVB-3664

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TVB-3664 Fatty Acid Synthase inhibitor

Cat.No.S8563

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 Fatty Acid Synthase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 468.47

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (200.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight 468.47 Formula

C25H23F3N4O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2097262-58-1 -- Storage of Stock Solutions

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
FASN
(mouse cell palmitate synthesis)
0.012 μM
FASN
(human cell palmitate synthesis)
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. This compound combined with taxane treatment enhances inhibition of in vitro tumor cell growth compared to treatmentwith either agent alone.
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.
References

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