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

Vistusertib (Synonyms: AZD2014)

Cat. No.: HY-15247 Purity: 98.82%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 92 In-stock
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Customer Review

Based on 15 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Vistusertib purchased from MCE. 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

    Vistusertib 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.

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

    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 MCE. Usage Cited in: Oncotarget. 2017 Feb 21;8(8):12775-12783.

    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 MCE. Usage Cited in: Oncotarget. 2018 Sep 21;9(74):33995-34008.

    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.

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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

    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].

    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].

    Clinical Trial
    Molecular Weight

    462.54

    Formula

    C₂₅H₃₀N₆O₃

    CAS No.

    1009298-59-2

    SMILES

    O=C(NC)C1=CC=CC(C2=CC=C3C(N=C(N4[[email protected]@H](C)COCC4)N=C3N5[[email protected]@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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (108.10 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.2162 mL 1.0810 mL 2.1620 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 98.82%

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    KeyWords:

    Vistusertib | AZD2014 | AZD 2014 | AZD-2014 | mTOR | Apoptosis | Autophagy | Mammalian target of Rapamycin | Inhibitor | inhibitor | inhibit

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