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BEZ235

Cat. No. M1671

All AbMole products are for research use only, cannot be used for human consumption.

BEZ235 Structure
Synonym:

NVP-BEZ235, Dactolisib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 30  USD30 In stock
50mg USD 65  USD65 In stock
100mg USD 100  USD100 In stock
200mg USD 145  USD145 In stock
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Quality Control & Documentation
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.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Biol Ther (2018). Figure 3. BEZ235 (AbMole BioScience)
Method CCK-8 assay
Cell Lines RCC 786-0 cell line
Concentrations 10 mmol/L
Incubation Time 48 or 72 h
Results These IC50 values were obviously lower than that of the compounds BEZ235 and BKM120, which may be promising candidates for development as new drugs targeting the PI3K pathway.
Source Apoptosis (2018). Figure 6. NVP-BEZ235 (Abmole Bioscience. USA)
Method Western Blot
Cell Lines HT29 and SW480 cells
Concentrations 96 nmol/l
Incubation Time 24 h
Results Resembling the WB results from the BZA treatment, the inhibitors AG490, NVP-BEZ23 and AZD6244 imitated BZA function, down-regulating the pivotal protein of the JAK/STAT3, PI3K/AKT/mTOR and Ras/Raf/MEK/ERK signal pathways
Source Apoptosis (2018). Figure 5. NVP-BEZ235 (Abmole Bioscience. USA)
Method cell apoptosis assay
Cell Lines HT29 and SW480 cells
Concentrations 96 nmol/l
Incubation Time 24 h
Results In addition, using the respective AG490 (50 μmol/l), NVP-BEZ235 (96 nmol/l) and AZD6244 (32 μmol/l) inhibitors for 24 h to mimic the BZA effect in colon cancer cells, we observed that the Bad/Bcl-2 ratio was significantly up-regulated and that Ki-67 mRNA expression was substantially down-regulated in this treatment group compared with the control group
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.
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.
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.
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.
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.
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.
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).
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 469.55
Formula C30H23N5O
CAS Number 915019-65-7
Solubility (25°C) DMSO 3 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Civallero et al. Expert Opin Investig Drugs. NVP-BEZ235 alone and in combination in mantle cell lymphoma: an effective therapeutic strategy.

[2] Karar et al. Cancer Biol Ther. Dual PI3K/mTOR inhibitor NVP-BEZ235 suppresses hypoxia-inducible factor (HIF)-1α expression by blocking protein translation and increases cell death under hypoxia.

[3] Roberts et al. Clin Cancer Res. Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models.

[4] Lin et al. J Chromatogr B Analyt Technol Biomed Life Sci. 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.

[5] Sally K Martin, et al. J Bone Miner Res. NVP-BEZ235, a dual pan class I PI3 kinase and mTOR inhibitor, promotes osteogenic differentiation in human mesenchymal stromal cells

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

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