1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    mTOR
    Autophagy
  3. Dactolisib Tosylate

Dactolisib Tosylate (Synonyms: BEZ235 (Tosylate); NVP-BEZ 235 (Tosylate))

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

Dactolisib Tosylate (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. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

For research use only. We do not sell to patients.

Dactolisib Tosylate Chemical Structure

Dactolisib Tosylate Chemical Structure

CAS No. : 1028385-32-1

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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
50 mg USD 72 In-stock
Estimated Time of Arrival: December 31
100 mg USD 108 In-stock
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200 mg USD 180 In-stock
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500 mg USD 360 In-stock
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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Dactolisib Tosylate:

Top Publications Citing Use of Products

    Dactolisib 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.

    Dactolisib 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.

    Dactolisib 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.

    Dactolisib Tosylate purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 9;37(1):188.

    Representative images of the western blotting analysis of TSSC3, ATG5, P62, LC3, Src, Akt, mTOR and their phosphorylated versions in MTF and SaOS2 cells. Cells are treated with TSSC3-overexpression, IGF-1, p-YEEI, and BEZ235 separately or in combination.

    Dactolisib Tosylate purchased from MCE. Usage Cited in: Biomed Res Int. 2018 Aug 5;2018:8372085.

    Changes of p-AKT and p-p70 S6K proteins after treatment with NVP-BEZ235 in Ishikawa and Ishikawa-TAX cells. Changes of p-AKT and p-p70 S6K proteins after treatment of Ishikawa and Ishikawa-TAX cells with NVP-BEZ235.
    • Biological Activity

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    • References

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    Description

    Dactolisib Tosylate (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. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

    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)

    mTORC1

     

    mTORC2

     

    Autophagy

     

    In Vitro

    Dactolisib (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 Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM[1].

    In Vivo

    Dactolisib (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, Dactolisib (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
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 34 mg/mL (52.98 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1 mg/mL (1.56 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    Mice: The NVP-Dactolisib (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
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    Keywords:

    DactolisibBEZ235NVP-BEZ 235BEZ 235BEZ-235PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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