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TVB-3664 is a 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. TVB-3664 combined with taxane treatment enhances inhibition of in vitro tumor cell growth compared to treatmentwith either agent alone. 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.
| Cell Experiment | |
|---|---|
| Cell lines | Calu-6 cells, A549 cells |
| Preparation 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. |
| Concentrations | 50 nM |
| Incubation time | 48 h, 72 h |
| Animal Experiment | |
|---|---|
| Animal models | female BALB-c-nude mice |
| Formulation | formulated at 3-V Biosciences in 100% PEG-400 and diluted with water to a final PEG concentration of 30% immediately before dosing for oral dosing |
| Dosages | 10 mg/kg, 2.5 mg/kg |
| Administration | PO, IV |
| Molecular Weight | 468.47 |
| Formula | C25H23F3N4O2 |
| CAS Number | 2097262-58-1 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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|---|
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| GSK837149A
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer. |
| IPI-9119
IPI-9119 is an orally active, selective and irreversible Fatty Acid Synthase (FASN) inhibitor, with an IC50 of 0.3 nM. |
| Eicosapentaenoic acid ethyl ester
Eicosapentaenoic acid ethyl ester (AMR101, EPA ethyl ester, Ethyl eicosapentaenoate) is an omega-3 fatty acid agent that significantly reduces the triglyceride (TG) levels and improves other lipid parameters without significantly increasing the low-density lipoprotein (LDL) cholesterol levels. |
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Products are for research use only. Not for human use. We do not sell to patients.
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