2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. mTOR Autophagy Apoptosis
  4. Vistusertib

Vistusertib  (Synonyms: AZD2014)

Cat. No.: HY-15247 Purity: 98.91%
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Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

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

Vistusertib Chemical Structure

Vistusertib Chemical Structure

CAS No. : 1009298-59-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 300 In-stock
100 mg USD 480 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 30 publication(s) in Google Scholar

Vistusertib Related Antibodies

Top Publications Citing Use of Products

    Vistusertib purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53.  [Abstract]

    Combination of RAD001 with AZD2281 (left panel) and AZD2014 with AZD2281 (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.

    Vistusertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Sep 21;9(74):33995-34008.  [Abstract]

    The treatment groups incorporating Selumetinib effectively blocks downstream p-ERK1/2 signaling, AZD2014 has a marked reduction in downstream mTORC1/2 effectors p-AKT, p-S6RP and p-4EBP1, and blockade of RICTOR.

    Vistusertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.  [Abstract]

    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.

    Vistusertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 21;8(8):12775-12783.  [Abstract]

    OSI-027, AZD-8055 and AZD-2014 almost completely block MHY1485-induced mTOR activation (p-mTOR/S6K1/Akt Ser473) in skin keratinocytes.

    Vistusertib purchased from MedChemExpress. Usage Cited in: Patent. US20160089377A1.

    Western blot of cortical extracts from Cntnap2 mutant or wild-type mice treated with vehicle or various mTOR pathway inhibitors, showing staining for the presence of phosphorylated S6. Individual mice are tested, and are represented in the lanes as follows. Lane 1=Cntnap2+/− mouse 9-10 weeks old treated with vehicle as for AZD2014; Lane 2=Cntnap2+/− mouse 7.3 months old treated with Rapamycin; Lane 3=Cntnap2+/− mouse 6.3 months old treated with Torin 2; Lane 4=Cn

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    mTOR mTORC1 mTORC2

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    • Protocol

    • Purity & Documentation

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    Description

    Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

    IC50 & Target[1]

    mTOR

    2.81 nM (IC50)

    mTORC1

     

    mTORC2

     

    PI3Kα

    3.766 μM (IC50)

    Autophagy

     

    In Vitro

    The inhibitory effects of Vistusertib (AZD2014) are measured against isolated recombinant mTOR enzyme (IC50 of 2.81 nM) as well as in cellular assays measuring both mTORC1 and mTORC2 activities. In MDAMB468 cells, Vistusertib (AZD2014) decreases the phosphorylation of the mTORC1 substrate ribosomal protein S6 (Ser235/236) with a mean IC50 value of 210 nM and the mTORC2 substrate AKT (Ser473) with a mean IC50 value of 78 nM[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Vistusertib Related Antibodies
    In Vivo

    Vistusertib (AZD2014) induces dose-dependent tumor growth inhibition in several xenograft and primary explant models. The antitumor activity of Vistusertib (AZD2014) is associated with modulation of both mTORC1 and mTORC2 substrates, consistent with its mechanism of action. The pharmacokinetics of Vistusertib (AZD2014) in mice is tested upon administration of doses between 7.5 and 15 mg/kg. A dose-dependent increase in Cmax and AUC is observed following single dose and repeat dosing of AZD2014: Cmax range from 1 to 16 μM and AUC range from 220 to 5,042 μM·h across this dose range. The pharmacodynamic effect of Vistusertib (AZD2014) against an mTORC1 biomarker (phosphorylation of S6) and an mTORC2 biomarker (phosphorylation of AKT) is assessed in SCID mice bearing MCF7 xenografts following administration of 3.75, 7.5, and 15 mg/kg AZD2014. There is a good relationship between the drug plasma concentrations and biomarker levels (estimated p-AKT IC50 of 0.119 μM total, 53% SE, and estimated p-S6 IC50 0.392 μM, 28.8% SE)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    462.54

    Formula

    C25H30N6O3
    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(NC)C1=CC=CC(C2=CC=C3C(N=C(N4[C@@H](C)COCC4)N=C3N5[C@@H](C)COCC5)=N2)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (108.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1620 mL 10.8099 mL 21.6198 mL
    5 mM 0.4324 mL 2.1620 mL 4.3240 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.40 mM); Suspended solution; Need ultrasonic and warming

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.91%

    COA (249 KB) LCMS (101 KB) Elemental Analysis Report (107 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    MCF7 experiments: 5×106 MCF7 cells are injected s.c. in a volume of 0.1 mL in male SCID mice and are randomized into control and treatment groups when tumor size reach 0.2 cm3. Vistusertib (AZD2014) is dissolved in captisol, and diluted to a final captisol concentration of 30% (w/v). Vistusertib (AZD2014) is administered by oral gavage (0.1 mL/10 g body weight). The control group receive vehicle only. Tumor volumes (measured by calliper), animal body weight and condition are recorded twice weekly for the duration of the study. The tumor volume is calculated (taking length to be the longest diameter across and width to be the corresponding perpendicular diameter) using the formula: (length×width)×√(length×width)×(π/6).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1620 mL 10.8099 mL 21.6198 mL 54.0494 mL
    5 mM 0.4324 mL 2.1620 mL 4.3240 mL 10.8099 mL
    10 mM 0.2162 mL 1.0810 mL 2.1620 mL 5.4049 mL
    15 mM 0.1441 mL 0.7207 mL 1.4413 mL 3.6033 mL
    20 mM 0.1081 mL 0.5405 mL 1.0810 mL 2.7025 mL
    25 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1620 mL
    30 mM 0.0721 mL 0.3603 mL 0.7207 mL 1.8016 mL
    40 mM 0.0540 mL 0.2702 mL 0.5405 mL 1.3512 mL
    50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0810 mL
    60 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9008 mL
    80 mM 0.0270 mL 0.1351 mL 0.2702 mL 0.6756 mL
    100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5405 mL
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    Vistusertib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vistusertib1009298-59-2AZD2014AZD 2014AZD-2014mTORAutophagyApoptosisMammalian target of RapamycinInhibitorinhibitorinhibit

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