KU-0063794 is a potent and selective mTOR inhibitor with IC50 values of approximately 10 nM for mTORC1 and mTORC2.But KU-0063794 does not inhibit the activity of 76 other protein kinases and seven lipid kinases at 1000-fold higher concentrations. KU-0063794 also inhibited growth of T47D breast cancer cells with a GI50 of 0.35 µM.
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Source | J Invest Dermatol (2013). Figure 1. KU-0063794 |
| Method | In-Cell Western Blotting | |
| Cell Lines | Primary KFs cells | |
| Concentrations | 10 μmol/l | |
| Incubation Time | 24 h | |
| Results | Both AZ compounds showed a significant (P<0.01) reduction of p-mTOR, Rictor, and Raptor immunoreactivity |
| Cell Experiment | |
|---|---|
| Cell lines | MEFs cell line |
| Preparation method | Cell growth. MEFs were seeded in 24-well plates (20000 cells per 1.91 cm2 well) and grown overnight in the presence of 10% foetal bovine serum. Cells were then treated in the presence or absence or rapamycin or Ku-0063794 and the medium was changed every 24 h with freshly dissolved inhibitors. Every 24 h of treatment, cells were washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 min. After washing once with water, the cells were stained with 0.1% Crystal Violet in 10% ethanol for 20 min and washed three times with water. Crystal Violet was extracted from cells with 0.5 ml of 10% (v/v) ethanoic (acetic) acid for 20 min. The eluate was then diluted 1:10 in water, and absorbance at 590 nm was quantified. |
| Concentrations | 3 μM |
| Incubation time | 1, 2 or 3 days |
| Animal Experiment | |
|---|---|
| Animal models | Xenograft Model of RCC |
| Formulation | solubilized in one part DMSO and then diluted (200 µg/100 µl) with 4 parts PEG1500 (50% (w/v) in 75 mM Hepes, pH 8.0, Roche Applied Science) |
| Dosages | 8 mg/kg once daily (five days a week) |
| Administration | intraperitoneal (IP) injection |
| Molecular Weight | 465.54 |
| Formula | C25H31N5O4 |
| CAS Number | 938440-64-3 |
| 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 |
| 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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