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BEZ235

Cat. No. M1671
BEZ235 Structure
Synonym:

NVP-BEZ235

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
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
Customer Product Validations & Biological Datas
Source Cell Death & Disease (2018). Figure 6. BEZ235 (Abmole Bioscience)
Method IHC analysis
Cell Lines Tumor-bearing nude mice
Concentrations 15 mg/kg
Incubation Time 4 weeks
Results Following BEZ235 treatment with or without ABT263, the expression of MCL-1 was suppressed while PUMA was increased; correspondingly, the expressions of p-AKT and p-4EBP1 were significantly suppressed.
Rating
Source Cell Death & Disease (2018). Figure 5. BEZ235 (Abmole Bioscience)
Method oral gavage
Cell Lines Tumor-bearing nude mice
Concentrations 15 mg/kg
Incubation Time 4 weeks
Results Our results showed that combination therapy of BEZ235 and ABT263 significantly suppressed tumor growth, comparing with each drug treatment alone.
Rating
Source Cell Death & Disease (2018). Figure 4. BEZ235 (Abmole Bioscience)
Method CO-IP analysis
Cell Lines MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
Concentrations 1 μM
Incubation Time 24 h
Results BIM and BAK were obviously released to trigger apoptosis once MCL-1 was suppressed by adding BEZ235 in the presence of ABT-263. Of note, although PUMA was upregulated by BEZ235, less PUMA was bound to MCL-1 than control group due to inhibition of MCL-1.
Rating
Source Cell Death & Disease (2018). Figure 3. BEZ235 (Abmole Bioscience)
Method Immunoblotting analysis
Cell Lines MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
Concentrations 1 μM
Incubation Time 24 h
Results We found that, besides MCL-1, the expression of PUMA but not other members was significantly increased following treatment of BEZ235 with or without ABT263 in MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells.
Rating
Source Cell Death & Disease (2018). Figure 2. BEZ235 (Abmole Bioscience)
Method colony formation assays
Cell Lines MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
Concentrations 1 μM
Incubation Time 24 h
Results The results showed that AZD8055 or BEZ235 in combination with ABT263 strongly inhibited cell proliferation in different TNBC cell lines.
Rating
Source Cell Death & Disease (2018). Figure 1. BEZ235 (Abmole Bioscience)
Method Immunoblotting analysis
Cell Lines TNBC cell lines
Concentrations 1 μM
Incubation Time 24 h
Results We found the mTOR inhibitors, especially the BEZ235 and AZD8055, could significantly inhibit the phosphorylation of AKT and 4EBP1 and efficiently led to decreasing MCL-1 expression.
Rating
Source Oncol Rep (2014). Figure 2. BEZ235
Method apoptosis assay
Cell Lines OCCC cells
Concentrations 10 and 100 nM
Incubation Time 72 h
Results OVISE cells were arrested at the G1 phase, but did not exhibit apoptosis (denoted by an increased proportion of cells in sub-G1), after 72 h of treatment with 10 and 100 nM NVP-BEZ235 (Fig. 2A).
Rating
Source Oncol Rep (2014). Figure 1. BEZ235
Method Western blot
Cell Lines OVISE cells
Concentrations 10 and 100 nM
Incubation Time 6 or 24 h
Results Treatment with NVP-BEZ235 suppressed pAKT expression, while treatment with temsirolimus did not. Similar results were observed in the KK cells.
Rating
Product Citations
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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  Catalog
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Keywords: BEZ235, NVP-BEZ235 supplier, PI3K, inhibitors

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