Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1min, without affecting the ability of class I PI3K to regulate Akt. It can also induce a rapid ~50-60% loss of SGK3 phosphorylation within 1min. VPS34-IN1 has no inhibition to the SGK2 isoform that does not possess a PtdIns(3)P-binding PX domain.
 |
Source | Biochem J (2014). Figure 3. VPS34-IN1 |
| Method | Immunofluorescence and time-lapse microscopy | |
| Cell Lines | U2OS cell line | |
| Concentrations | 1.0 μM | |
| Incubation Time | 1 h | |
| Results | Treatment with Vps34-IN1 for 1 h induced a marked dose-dependent suppression of endosomal localization of GFP–2×FYVEHrs with ~80% loss observed at 1.0 μM and ~50% loss at 0.1 μM |
| Molecular Weight | 425.91 |
| Formula | C21H24ClN7O |
| CAS Number | 1383716-33-3 |
| Solubility (25°C) | 65 mg/mL in DMSO |
| 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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