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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $39 | In Stock | |
50 mg | $52 | In Stock | |
100 mg | $64 | In Stock | |
200 mg | $108 | In Stock |
Description | Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110 |
Targets&IC50 | p110 |
In vitro | Dactolisib (BEZ235) shows slightly lower activity against the |
In vivo | In the absence of inhibitors, the weight of the chamber, as well as levels of the endothelial cell marker Tie-2, were significantly increased in the presence of VEGF. Both effects were significantly inhibited in a dose-dependent manner when the mice were treated with NVP-BEZ235 given p.o. twice a day at 20 mg/kg or once at 30 mg/kg, showing the specificity of the angiogenic response driven by the VEGF [2]. NVP-BEZ235–treated adenomas (20 mg/kg) showed pronounced vacuolation of the cytoplasm when compared with PEG-treated animals. Vacuoles appeared even more prominent at the 30 and 45 mg/kg doses [3]. |
Kinase Assay | PI3K |
Cell Research | The proliferation of BON1, QGP1, and |
Animal Research | Three doses of NVP-BEZ235 were tested in MENX rats: 20, 30, and 45 mg/kg. As the two higher doses caused a weight loss >10% after 10 days of treatment, the dose of 20 mg/kg was used for further studies. For MRI studies, MENX-affected rats at 7 to 8 months of age (with sizeable adenomas but still in good general health) were treated for 14 days with NVP-BEZ235 (20 mg/kg) or placebo (PEG) administered daily per oral gavage. The side effect of the drug we observed was mild diarrhea in the last days of the treatment (4/8 rats). Being this our first in vivo study of spontaneous rat pituitary adenomas, functional/molecular changes in the tumors were considered more objective and measurable endpoints (primary endpoints) compared to the size and/or survival (secondary endpoints) [3]. |
Alias | BEZ235, NVP-BEZ235 |
Molecular Weight | 469.54 |
Formula | C30H23N5O |
Cas No. | 915019-65-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: 1 mg/ml, Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) |
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