Chemical structure of NVP-BEZ235.
Western blot analysis of extracts from Jurkat cells, untreated or treated with NVP-BEZ235 (2 hr) at the indicated concentrations. The phosphorylation of p70 S6 kinase was detected using Phospho-p70 S6 Kinase (Thr389) (108D2) Rabbit mAb #9234 (upper) and p70 S6 Kinase (49D7) Rabbit mAb #2708 (lower).
Western blot analysis of extracts from Jurkat cells, untreated or treated with NVP-BEZ235 (2 hr) at the indicated concentrations. The phosphorylation of Akt was detected using Phospho-Akt (Ser473) (D9E) XP® Rabbit mAb #4060 (upper) and Akt (pan) (C67E7) Rabbit mAb #4691 (lower).
NVP-BEZ235 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.065 ml DMF and warm to 75°C for 5 minutes. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5 nM-500 nM for 2-24 hr.
Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Solubility: Soluble in DMF at 10 mg/ml with warming. Soluble in DMSO at 1.33 mg/ml with warming. Very poorly soluble in water and ethanol.
|Solubility||Soluble in anhydrous DMF at 10mg/ml and DMSO at 1.33mg/ml.|
NVP-BEZ235 is a selective and potent dual inhibitor of PI3 kinase and mTOR Ser/Thr protein kinase. Research studies show that NVP-BEZ235 reversibly inhibits the catalytic activity of these kinases by competing with ATP at the ATP-binding site (1,2). Studies demonstrate that NVP-BEZ235 has anti-proliferative characteristics and induces cell cycle arrest during G0/G1 phase through inhibition of CDK4 and cyclin D3 (2,3).
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