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BGT226 (NVP-BGT226) is a novel phosphoinositide 3-kinase/mTOR dual inhibitor. BGT226 (NVP-BGT226) displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.
| Cell Experiment | |
|---|---|
| Cell lines | FaDu, Detroit 562, HONE-1 and HONE-1-C15 cells line |
| Preparation method | Growth-inhibition assay. Cells in the logarithmic growth phase were cultured at a density of 5,000 to 20,000 cells per milliliter per well in a 24-well plate. The cells were exposed to various concentrations of BGT226 for 3 generation times. At the end of the incubation period, cells were fixed and stained with 50% ethanol containing 0.5% methylene blue for 30 minutes. The resulting colored residues were dissolved in 1% N-lauroyl-sarcosine, and optical density was read at 550 nm using a microplate reader. The IC50 value resulting from 50% inhibition of cell growth was calculated graphically as a comparison with control groups. Each point represents the average of at least 3 independent experiments run in duplicate. |
| Concentrations | IC50 ranging from 7.4 to 30.1 nmol/L |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | human FaDu xenografted mice |
| Formulation | dissolved in 90% N-methyl-2-pyrrolidone (NMP)/10% PEG300 |
| Dosages | 3.5 and 5mg/kg once a day for 21 consecutive days |
| Administration | orally |
| Molecular Weight | 650.6 |
| Formula | C32H29F3N6O6 |
| CAS Number | 1245537-68-1 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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