TVB-3664 is a FASN inhibitor which 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 | |
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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 | |
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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 85 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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