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V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
| Cell Experiment | |
|---|---|
| Cell lines | HCC1806 cells |
| Preparation method | Immunofluorescence HCC1806 cells were treated V-9302 (25 µM aqueous, 1% DMSO) for 48 h. Following treatment, cells were fixed with 70% methanol for 5-10 min. LC3B was visualized with 1:100 primary antibody (anti LC3B) at 37 ºC for 45 min followed by application of 1:600 secondary antibody (Rhodamine Red) at 37 ºC for 30 min and DAPI for 4 min. Images were acquired with a fluorescence microscope at visualized at 40× magnification. |
| Concentrations | 25 µM aqueous, 1% DMSO |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | 6-week old, female athymic nude mice bearing HCT-116 (KRASG13D) or HT29 (BRAFV600E) cell-line xenografts |
| Formulation | reconstituted in a vehicle of phosphate buffered saline supplemented with 2% DMSO |
| Dosages | 75 mg/kg per day for 21 days |
| Administration | intraperitoneally |
| Molecular Weight | 575.14 |
| Formula | C34H39ClN2O4 |
| CAS Number | 2416138-42-4 |
| Solubility (25°C) | DMSO 100 mg/mL Water 50 mg/mL |
| Storage | 2-8°C, dry, sealed |
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