BEZ235 (NVP-BEZ235) is a dual inhibitor of the PI3K and the downstream mammalian target of rapamycin (mTOR) by binding to the ATP-binding cleft of these enzymes. It inhibited the activation of the downstream effectors Akt, S6 ribosomal protein, and 4EBP1 in breast cancer cells. For Class I PI3K family, its biochemical IC50 is 4nM against p110α, 75nM against p110β, 7nM against p110σ, 5nM against p110γ. Quantification of S473-Akt and T308P-Akt levels by ELISA revealed that 50% reduction occurred at a compound concentration of 8.0 nM and 30 nM.
Technical information:
| Chemical Formula: | C30H23N5O | |
| CAS #: | 915019-65-7 | |
| Molecular Weight: | 469.54 | |
| Purity: | >98% | |
| Appearance: | Pale white solid | |
| Chemical Name: | 2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo [4,5-c]quinolin-1-yl)phenyl)propanenitrile | |
| Solubility: | Up to 100 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Sauveur-Michel Maira et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol. Cancer Ther. 7: 1851 (2008). |
| 2. | Violeta Serra et al. NVP-BEZ235, a Dual PI3K/mTOR Inhibitor, Prevents PI3K Signaling and Inhibits the Growth of Cancer Cells with Activating PI3K Mutations. Cancer Res. 68: 8022 (2008). |
Other Information:
Product Specification (pdf)
MSDS (pdf)
