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BEZ235

Cat. No. M1671
BEZ235 Structure
Synonym:

NVP-BEZ235

Size Price Availability Quantity
50mg USD 55 In stock
200mg USD 120 In stock
500mg USD 240 In stock
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Quality Control
Biological Activity

BEZ235 (NVP-BEZ235) is a potent dual inhibitor of PI3K and mTOR. BEZ235 (NVP-BEZ235) is able to effectively and specifically block the dysfunctional activation of the PI3K pathway and induce G (1) arrest. It also inhibits the growth of human cancer in animal models. For Class I PI3K family, NVP-BEZ235 biochemical IC50 are 4nM against p110α, 75nM against p110β, 7nM against p110σ, 5nM against p110γ.

Protocol
Cell Experiment
Cell lines MKN45, BT474, SNU216 and NCI-N87 cell lines
Preparation method Cell viability assay Cells were seeded at a density of 2000 cells per well in a 96-well plate and incubated overnight in complete medium. Cells were treated with either trastuzumab, BEZ235, Everolimus, AZD6244 alone, or trastuzumab combined with BEZ235 or Everolimus or AZD6244. After 72 h of incubation, cell viability was determined using the MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay, Promega, Madison, WI, USA) following the manufacturer’s instructions. The absorbance was measured at 490 nm using a spectrophotometer. All experiments were repeated three times with at least triplicate readings for each concentration.
Concentrations 0~800nM
Incubation time 72h
Animal Experiment
Animal models Xenograft models in non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice
Formulation BEZ235 was formulated in 0.9 % NaCl as a homogeneous suspension (9 mg/mL) and stored at 4 °C until further use in the in vivo experiments.
Dosages 45 mg/kg body weight, daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 469.55
Formula C30H23N5O
CAS Number 915019-65-7
Purity 99.16%
Solubility DMSO
Storage at -20°C
References

NVP-BEZ235 alone and in combination in mantle cell lymphoma: an effective therapeutic strategy.
Civallero et al. Expert Opin Investig Drugs. 2012 Aug 25. PMID: 22920938.

Dual PI3K/mTOR inhibitor NVP-BEZ235 suppresses hypoxia-inducible factor (HIF)-1α expression by blocking protein translation and increases cell death under hypoxia.
Karar et al. Cancer Biol Ther. 2012 Sep 1;13(11). PMID: 22895065.

Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models.
Roberts et al. Clin Cancer Res. 2012 Aug 7. PMID: 22872574.

Determination of NVP-BEZ235, a dual PI3K and mTOR inhibitor, in human and mouse plasma and in mouse tissue homogenates by reversed-phase high-performance liquid chromatography with fluorescence detection.
Lin et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Jul 15;901:9-17. PMID: 22727754.

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Keywords: BEZ235, NVP-BEZ235 supplier, PI3K, inhibitors

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