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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 |
| Related FAS Products |
|---|
| C75
C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS). C75 inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator. |
| Orlistat
Orlistat is an irreversible inhibitor of pancreatic and gastric lipases with IC50 of 122 ng/ml for PL from human duodenal juice. |
| Betulin
Betulin is a specific, small molecule inhibitor of SREBP (Sterol Regulatory Element-Binding Proteins). |
| Pseudoprotodioscin
Pseudoprotodioscin, a furan glucoside, inhibits sREBP1/2 and microRNA 33A/B levels and reduces the expression of genes associated with cholesterol and triglyceride synthesis. |
| Albaspidin-AP
Albaspidin AP inhibited fatty acid synthase (FAS) with IC50 value of 71.7 μM. Fatty acid synthase is emerging as a potential therapeutic target for cancer and obesity. |
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