1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    mTOR
    Autophagy

BEZ235 Tosylate (Synonyms: NVP-BEZ 235 Tosylate)

Cat. No.: HY-15174 Purity: 99.89%
Handling Instructions

BEZ235 Tosylate is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively.

For research use only. We do not sell to patients.
BEZ235 Tosylate Chemical Structure

BEZ235 Tosylate Chemical Structure

CAS No. : 1028385-32-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
50 mg USD 72 In-stock
100 mg USD 108 In-stock
200 mg USD 180 In-stock
500 mg USD 360 In-stock
1 g   Get quote  
5 g   Get quote  

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Other Forms of BEZ235 Tosylate:

    BEZ235 Tosylate purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    BEZ235 Tosylate purchased from MCE. Usage Cited in: Leukemia. 2014 Sep;28(9):1819-27.

    Western blot analysis of human T-ALL cell lines treated for 24 hours using DMSO (vehicle control), 1 μM JQ1, 500 nM BEZ235, or both drugs in combination, using the indicated antibodies. Western blot analysis of these T-ALL cell lines following treatment with JQ1, BEZ235 or both drugs in combination reveals cooperative upregulation of BIM protein expression coupled to induction of apoptosis, as assessed by PARP cleavage.

    BEZ235 Tosylate purchased from MCE. Usage Cited in: EBioMedicine. 2015 Nov 19;2(12):1944-56.

    SW620 xenograft tumors are treated with SB202190 and OSI027 individually or in combination. The effect on signaling by p38 (P-MK2 and P-Hsp27) and mTOR (P-S6K1 and P-AKT) is analyzed by immunoblot. SB202190 achieves on-target inhibition by diminishes phosphorylation of MK2 and Hsp27. OSI-027 blocks signaling by both mTORC1 and mTORC2 by decreases phosphorylation of S6K1 and AKT. When SB202190 and OSI-027 are used in combination, all three kinases, p38, mTORC1 and mTORC2 are potently inhibited.

    BEZ235 Tosylate purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45470-45483.

    Activity of PI3K/AKT/mTOR is monitored by examining phosphorylation of AKT-S473, AKT-T308, and S6 by western blotting.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BEZ235 Tosylate is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively.

    IC50 & Target[1]

    p110α

    4 nM (IC50)

    p110α-H1047R

    4.6 nM (IC50)

    p110α-E545K

    5.7 nM (IC50)

    p110γ

    5 nM (IC50)

    p110δ

    7 nM (IC50)

    p110β

    75 nM (IC50)

    mTOR

    20.7 nM (IC50)

    Autophagy

     

    In Vitro

    NVP-BEZ235 is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of NVP-BEZ235, with an average GI50 of 10 to 12 nM[1].

    In Vivo

    NVP-BEZ235 is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, NVP-BEZ235 appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[1].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.5583 mL 7.7913 mL 15.5826 mL
    5 mM 0.3117 mL 1.5583 mL 3.1165 mL
    10 mM 0.1558 mL 0.7791 mL 1.5583 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    NVP-BEZ235 is dissolved in DMSO to a stock concentration of 10 mM and diluted with cell media. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 nL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110γ, and p110δ, respectively) are then added. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and ran for either 60 or 120 min and subsequently terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: The NVP-BEZ235 powder is dissolved in NMP on sonication, and the remaining volume of polyethylene glycol 300 is added to a concentration of 5 mg/mL. The application volume is 10 mL/kg. For analytics, frozen tissues are minced and then homogenized in an equal volume of ice-cold PBS and centrifugation, supernatants are analyzed. Samples are then eluted with a linear gradient of 10% to 90% (v/v) acetonitrile in water containing 0.05% (v/v) trifluoroacetic acid over a period of 20 min at a flow rate of 1 mL/min. The compounds are detected by UV absorbance at 340 nm, and concentrations are determined by the external standard method using peak heights[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    641.74

    Formula

    C₃₇H₃₁N₅O₄S

    CAS No.

    1028385-32-1

    SMILES

    CN(C1=C2C3=CC(C4=CC5=CC=CC=C5N=C4)=CC=C3N=C1)C(N2C6=CC=C(C=C6)C(C)(C#N)C)=O.CC7=CC=C(S(=O)(O)=O)C=C7

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 34 mg/mL (Need ultrasonic and warming); H2O: < 1 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    BEZ235 Tosylate
    Cat. No.:
    HY-15174
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