2. PI3K/Akt/mTOR Autophagy
  3. Akt Autophagy
  4. Capivasertib

Capivasertib  (Synonyms: AZD5363)

Cat. No.: HY-15431 Purity: 99.95%
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Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.

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

Capivasertib Chemical Structure

Capivasertib Chemical Structure

CAS No. : 1143532-39-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
1 mg USD 38 In-stock
5 mg USD 96 In-stock
10 mg USD 144 In-stock
25 mg USD 260 In-stock
50 mg USD 360 In-stock
100 mg USD 480 In-stock
500 mg USD 1450 In-stock
1 g USD 2200 In-stock
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Customer Review

Based on 57 publication(s) in Google Scholar

Other Forms of Capivasertib:

Capivasertib Related Antibodies

Top Publications Citing Use of Products

56 Publications Citing Use of MCE Capivasertib

WB

    Capivasertib purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Jun;17(6):1349-1366.  [Abstract]

    MiaPaca2 cells are treated with 25 μM AZD5363 (AKT inhibitor), 0.1 μM AZD2014 (MTOR inhibitor) for 24 h. Expression of RPS6, p-RPS6, lipidated and non-lipidated MAP1LC3B and ACTB proteins are determined by immunoblotting.

    View All Akt Isoform Specific Products:

    View All Isoforms
    Akt Akt1 Akt2 Akt3

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.

    IC50 & Target[1]

    Akt1

    3 nM (IC50)

    Akt2

    7 nM (IC50)

    Akt3

    7 nM (IC50)

    P70S6K

    6 nM (IC50)

    PKA

    7 nM (IC50)

    ROCK2

    60 nM (IC50)

    ROCK1

    470 nM (IC50)

    Autophagy

     

    In Vitro

    Capivasertib, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less. Capivasertib inhibits phosphorylation of these substrates with an IC50 value of 0.06 to 0.76 μM in the 3 cell lines. Capivasertib effectively inhibits phosphorylation of S6 and 4E-BP1 in these cell lines, whereas it increases phosphorylation of AKT at both ser473 and thr308. In BT474c cells, Capivasertib induces FOXO3a nuclear translocation with EC50 value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus. AZD5363Capivasertibhibitor MK-2206 is much less active (IC50>30 μM)[1].

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

    Capivasertib Related Antibodies
    In Vivo

    Oral dosing of Capivasertib (AZD5363) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50 ~0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts[1].

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

    428.92

    Formula

    C21H25ClN6O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to gray

    SMILES

    O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
    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 : 125 mg/mL (291.43 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 2.3314 mL 11.6572 mL 23.3144 mL
    5 mM 0.4663 mL 2.3314 mL 4.6629 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)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

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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: ≥ 2.08 mg/mL (4.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.95%

    COA (256 KB) HNMR (300 KB) LCMS (97 KB)

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

    Cell proliferation assay is determined by 2 methods, MTS and Sytox Green. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37°C, 5% CO2. Cells are then exposed to concentrations of Capivasertib ranging from 30 to 0.003 μM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent. Absorbance is measured with a Tecan Ultra instrument. For the Sytox Green endpoint, Sytox Green nucleic acid dye diluted in TBS-EDTA buffer is added to cells (final concentration of 0.13 μM) and the number of dead cells detected using an Acumen Explorer. Cells are then permeabilized by the addition of saponin (0.03% final concentration, diluted in TBS-EDTA buffer), incubated overnight and a total cell count measured. Predose measurements are made for both MTS and Sytox Green endpoints, and concentration needed to reduce the growth of treated cells to half that of untreated cells (GI50) values are determined using absorbance readings (MTS) or live cell counts[1].

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

    Mice[1]
    Specific, pathogen-free, female nude mice (nu/nu: Alpk) and male SCID mice (SCID/CB17; 786-0 xenograft studies) are used. When mean tumor sizes reach approximately 0.2 cm3, the mice are randomized into control and treatment groups. The treatment groups received varying dose schedules of Capivasertib (AZD5363) solubilized in a 10% DMSO 25% w/v Kleptose HPB (Roquette) buffer by oral gavage, RP-56976 solubilized in 2.6% ethanol in injectable water by intravenous injection once on day 1 at 15 or 5 mg/kg once weekly. When administered in combination, RP-56976 is administered 1 hour before the oral dose of Capivasertib (AZD5363). The control group received the DMSO/Kleptose buffer alone, twice daily by oral gavage. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Mice are sacrificed by CO2 euthanasia. The tumor volume is calculated (taking length to be the longest diameter across the tumor and width to be the corresponding perpendicular diameter) using the formula: (length×width)×√(length×width)×(π/6). Growth inhibition from the start of treatment is assessed by comparison of the differences in tumor volume between control and treated groups.

    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 2.3314 mL 11.6572 mL 23.3144 mL 58.2859 mL
    5 mM 0.4663 mL 2.3314 mL 4.6629 mL 11.6572 mL
    10 mM 0.2331 mL 1.1657 mL 2.3314 mL 5.8286 mL
    15 mM 0.1554 mL 0.7771 mL 1.5543 mL 3.8857 mL
    20 mM 0.1166 mL 0.5829 mL 1.1657 mL 2.9143 mL
    25 mM 0.0933 mL 0.4663 mL 0.9326 mL 2.3314 mL
    30 mM 0.0777 mL 0.3886 mL 0.7771 mL 1.9429 mL
    40 mM 0.0583 mL 0.2914 mL 0.5829 mL 1.4571 mL
    50 mM 0.0466 mL 0.2331 mL 0.4663 mL 1.1657 mL
    60 mM 0.0389 mL 0.1943 mL 0.3886 mL 0.9714 mL
    80 mM 0.0291 mL 0.1457 mL 0.2914 mL 0.7286 mL
    100 mM 0.0233 mL 0.1166 mL 0.2331 mL 0.5829 mL
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    Capivasertib 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:

    Capivasertib1143532-39-1AZD5363AZD 5363AZD-5363AktAutophagyPKBProtein kinase BInhibitorinhibitorinhibit

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