1. PI3K/Akt/mTOR
  2. Akt
  3. Uprosertib

Uprosertib  (Synonyms: GSK2141795)

Cat. No.: HY-15965 Purity: 99.74%
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Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

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

Uprosertib Chemical Structure

Uprosertib Chemical Structure

CAS No. : 1047634-65-0

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
5 mg USD 99 In-stock
10 mg USD 165 In-stock
50 mg USD 457 In-stock
100 mg USD 759 In-stock
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Uprosertib:

Top Publications Citing Use of Products

    Uprosertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jul 31;9(59):31549-31558.  [Abstract]

    Western blots of the indicated proteins in the DMS114-P and DMS114-R cells treated with (+) and without (-) the AKT inhibitor, Uprosertib (200 nM) for 6 h (left panel) or 24 h (right panel). In the case of DMS114-P, extracts with (+) and without (-) treatment with PD173074 (1 µM) are also shown.

    Uprosertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Sep 4;8(1):410.  [Abstract]

    Effect of EGFR TKIs and Akt inhibitors on key signal transduction proteins in parental and resistant PC9 cells. Western blot analysis of PC9 and PC9-ER treated for 4 h with Erlotinib (30 µM), GSK2141795 (2.5 µM) or the combination.

    Uprosertib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Apr;16(4):614-624.  [Abstract]

    Western blot analysis is performed with lysates from resistant cell lines treated either with vehicle (DMSO) or GSK2141795 (1 μM) for 24 hours to assess inhibition of Akt (pAKT) and downstream (pGSK3) signaling (three experimental replicates).

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

    IC50 & Target[1]

    Akt3

    38 nM (IC50)

    Akt1

    180 nM (IC50)

    Akt2

    328 nM (IC50)

    ROCK1

    1570 nM (IC50)

    ROCK2

    1850 nM (IC50)

    CDK7

    2100 nM (IC50)

    In Vitro

    Uprosertib (GSK2141795) inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib (GSK2141795) in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

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

    Clinical Trial
    Molecular Weight

    429.25

    Formula

    C18H16Cl2F2N4O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (116.48 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 2.3296 mL 11.6482 mL 23.2964 mL
    5 mM 0.4659 mL 2.3296 mL 4.6593 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 (stored under nitrogen). 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 (5.82 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 (5.82 mM); Suspended solution; Need ultrasonic

      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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    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
    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 (stored under nitrogen). 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 2.3296 mL 11.6482 mL 23.2964 mL 58.2411 mL
    5 mM 0.4659 mL 2.3296 mL 4.6593 mL 11.6482 mL
    10 mM 0.2330 mL 1.1648 mL 2.3296 mL 5.8241 mL
    15 mM 0.1553 mL 0.7765 mL 1.5531 mL 3.8827 mL
    20 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9121 mL
    25 mM 0.0932 mL 0.4659 mL 0.9319 mL 2.3296 mL
    30 mM 0.0777 mL 0.3883 mL 0.7765 mL 1.9414 mL
    40 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4560 mL
    50 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
    60 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9707 mL
    80 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7280 mL
    100 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5824 mL
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    Uprosertib 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.

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    Product Name:
    Uprosertib
    Cat. No.:
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