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 |
| 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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