2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. mTOR Autophagy Apoptosis
  4. AZD-8055

AZD-8055 est un inhibiteur de la kinase mTOR qui est ATP-compétitif, puissant, sélectif et oralement biodisponible, avec un IC50 de 0,8 nM. AZD-8055 inhibe mTORC1 et mTORC2.

AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.

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

AZD-8055 Chemical Structure

AZD-8055 Chemical Structure

CAS No. : 1009298-09-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 45 In-stock
10 mg USD 66 In-stock
50 mg USD 145 In-stock
100 mg USD 238 In-stock
200 mg USD 436 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 60 publication(s) in Google Scholar

AZD-8055 Related Antibodies

Top Publications Citing Use of Products

49 Publications Citing Use of MCE AZD-8055

WB

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Mar 6.

    AZD8055 (100, 500, 1000 nM; 48h) significantly suppresses the expression of pAKT, p-S6K1 and p-mTOR in both the T24 and 5637 human bladder urothelial carcinoma cell lines, and the SCaBER and UM-UC-3 human bladder squamous cell carcinoma cell line.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ATL-43T cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ED-40415 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    MT-2 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    HUT-102 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 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.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45793-45806.  [Abstract]

    Cells are treated for 2 h with AZD8055 at the indicated concentrations (0, 50, 200 and 800 nM), and cell lysates are probed with phosphor- and total antibodies of mTOR signaling pathway. β-actin is used as loading control. Blot shown is representative of at least two independent experiments.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682.  [Abstract]

    CHP-212 and SK-N-AS cells are treated with indicated concentrations of AZD6244, MEK162, RAD001 or AZD8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot. Phosphorylation levels of AKT, ERK and S6 are detected by specific anti-phospho antibodies. Loading is verified by specific antibodies to total AKT, ERK and anti-tubulin.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.

    CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Dec 8;6(39):42183-96.  [Abstract]

    KNS-62 and T24 cells are treated with 250 nM AZD6244, 250 nM MEK162, 5 nM of RAD001, 250 nM AKT8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot.

    AZD-8055 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 Apr 15;73(8):2574-86.  [Abstract]

    Cells are treated with the indicated concentrations of AZD8055, Torin2 or staurosporin overnight and analyzed by western blot using antibodies specific for the indicated proteins.

    View All mTOR Isoform Specific Products:

    View All Isoforms
    mTOR mTORC1 mTORC2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2[1].

    IC50 & Target

    mTOR

    0.8 nM (IC50)

    mTORC1

     

    mTORC2

     

    Autophagy

     

    In Vitro

    The inhibitory activity of AZD-8055 (AZD8055) against mTOR is evaluated using two different assays. Using the truncated recombinant mTOR enzyme, the IC50 for AZD8055 is 0.13±0.05 nM. Using native mTOR enzyme complexes extracted from HeLa cells, the IC50 is 0.8±0.2 nM. AZD-8055 shows excellent selectivity (~1,000-fold) against all class I PI3K isoforms and other members of the PI3K-like kinase family. AZD-8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The cellular IC50s for AZD8055 are calculated as 24±9 nM (n=13) for pAKT Ser473 and 27±3 nM (n=12) for pS6 Ser235/236 in MDA-MB-468 cells[1].

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

    AZD-8055 Related Antibodies
    In Vivo

    In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD-8055 (AZD8055) results in a dose-dependent tumor growth inhibition of 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. A similar dose dependency is observed in nude mice bearing A549 xenografts: tumor growth inhibition is 44%, 55%, and 93% after 2.5, 5, and 10 mg/kg/d twice daily, respectively. AZD8055 also results in significant inhibition of tumor growth and/or regression in breast, lung, colon, prostate, and uterine xenograft models when administered either twice daily at 10 mg/kg or daily at a dose of 20 mg/kg[1]. AZD8055 markedly decreases the phosphorylation levels of mTOR and its substrates and the activation of microglia in vivo, and promotes the microglial polarization from M1 phenotype to M2 phenotype. In addition, administration of AZD8055 following subarachnoid hemorrhage (SAH) significantly ameliorates EBI, including neuronal apoptosis, neuronal necrosis, brain edema and blood-brain barrier permeability[2].

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

    465.54

    Formula

    C25H31N5O4
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OCC1=CC(C2=NC3=NC(N4CCOC[C@@H]4C)=NC(N5[C@@H](C)COCC5)=C3C=C2)=CC=C1OC
    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 : 33.33 mg/mL (71.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1480 mL 10.7402 mL 21.4804 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (10.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.37 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  30% SBE-β-CD in Saline

      Solubility: 50 mg/mL (107.40 mM); Clear solution; Need ultrasonic and adjust pH to 2 with HCl

    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: 99.60%

    COA (249 KB) HNMR (470 KB) LCMS (107 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Inhibition of mTOR is evaluated using two methodologies: The high-throughput assay uses an α screen capture complex technology with a recombinant truncated FLAG-tagged mTOR (amino acids 1362-2549; expressed in HEK293 cells) and a biotinylated p70 peptide substrate. In addition, native mTOR activity is assayed using immunoprecipitation of full-length mTOR from HeLa cytoplasmic extract, and the endogenous mTOR is in protein complexes with Rictor and Raptor. A kinase assay is performed in the presence of recombinant 4E-BP1 protein as substrate with detection of the phosphorylated product through an ELISA format. The activity of the lipid kinases, class I PI3Ks α, β, δ, and γ, is measured using recombinant PI3Ks with the lipid PIP2 as substrate. Assays for the ataxia-telangiectasia mutated (ATM) and DNA-PK are performed. Finally, counterscreen against 260 kinases is carried out at a fixed concentration of 10 μM AZD-8055[1].

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

    For growth inhibition and acridine staining, cells are exposed to increasing concentrations of AZD-8055 (0 to 1,280 nM) for 72 to 96 h and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images are captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells are quantified. For LC3 assessment, cells are exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells are lysed on ice and analyzed by immunoblotting[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Mice[1]
    Tumor cells (106 for U87-MG, 5×106 for A549) are injected s.c. in a volume of 0.1 mL, and mice are randomized into control and treatment groups when tumor size reach 0.2 cm3. AZD-8055 is administered by oral gavage (0.1 mL/10 g of body weight) once or twice daily. The control group receive the vehicle only. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated.
    Rats[2]
    Sprague-Dawley (SD) rats (250 g) and pregnant SD rats (16-18 days gestation, used for microglia extraction) are used. In experiment 1, 48 rats (54 rats are used, 48 rats survive after the surgery) are assigned randomly to four groups: sham group, SAH 3 h group, SAH 24 h group, SAH 72 h group. The animals in SAH 3 h, 24 h and 72 h groups are subjected to experimental SAH and are killed at 3 h, 24 h and 72 h after blood injection, respectively (n=12 for each group). In experiment 2, 72 rats (83 rats are used, 72 rats survive after the surgery) are assigned randomly to sham group (n=18), SAH+vehicle group (n=18), SAH+Rapamycin group (n=18), SAH+AZD8055 group (n=18). The rat receive a single intraperitoneal injection of Rapamycin immediately after induction of SAH, the dose of Rapamycin used is 150 μg/kg body weight. AZD8055 is administered by oral gavage with the dose of 14 mg/kg body weight. Rats in vehicle group are treated with equal volume solvent. All the rats in experiment 2 are killed at 24 h post-SAH. In experiment 3, enriched microglia are distributed into 5 groups: Control, OxyHb, OxyHb+vehicle (DMSO), OxyHb+Rapamycin and OxyHb+AZD8055. Twenty-four hours after microglia re-seeding, cells are treated with OxyHb (10 μM), DMSO (volume equal to Rapamycin and AZD8055), Rapamycin (2.74 mM), AZD8055 (0.8 nM) respectively in fresh medium. After incubation for 24 h (in 37°C, 5% CO2), cell medium is removed, washed by PBS for 3 times and fixed by 4% paraformaldehyde.

    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 2.1480 mL 10.7402 mL 21.4804 mL 53.7011 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 mL 10.7402 mL
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL 5.3701 mL
    15 mM 0.1432 mL 0.7160 mL 1.4320 mL 3.5801 mL
    20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6851 mL
    25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1480 mL
    30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    AZD-8055 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:

    AZD-80551009298-09-2AZD8055AZD 8055mTORAutophagyApoptosisMammalian target of RapamycinInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    AZD-8055
    Cat. No.:
    HY-10422
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.