1. PI3K/Akt/mTOR
  2. Akt
  3. GSK2110183

GSK2110183 

Cat. No.: HY-15966
Handling Instructions

GSK2110183 is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

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

GSK2110183 Chemical Structure

GSK2110183 Chemical Structure

CAS No. : 1047634-63-8

Size Price Stock
5 mg USD 420 Get quote
10 mg USD 600 Get quote
50 mg USD 1800 Get quote
100 mg USD 2520 Get quote

* Please select Quantity before adding items.

Other In-stock Forms of GSK2110183:

Other Forms of GSK2110183:

Top Publications Citing Use of Products

    GSK2110183 purchased from MCE. Usage Cited in: Theranostics. 2019 Jan 30;9(4):1096-1114.

    RAS signaling alterations induced by the AKT inhibitor GSK2110183 (10 nM; 8 h), showing that AKT signaling is mutually suppressive.

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK2110183 is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

    IC50 & Target[1]

    Akt1

    0.08 nM (Ki)

    Akt2

    2 nM (Ki)

    Akt3

    2.6 nM (Ki)

    Akt1 E17K mutant

    0.2 nM (IC50)

    PKG1α

    0.9 nM (IC50)

    PKA

    1.3 nM (IC50)

    PKG1β

    4 nM (IC50)

    ROCK

    100 nM (IC50)

    PKCη

    210 nM (IC50)

    P70S6K

    251 nM (IC50)

    RSK1

    316 nM (IC50)

    PKCβ1

    430 nM (IC50)

    PKCθ

    510 nM (IC50)

    In Vitro

    GSK2110183 is an ATP competitive, time dependant and fully reversible inhibitors of the Akt kinase family. GSK2110183 has a Ki of 0.08, 2 and 2.6 nM against Akt1, Akt2 and Akt3, respectively. GSK2110183 inhibits the kinase activity of the E17K Akt 1 mutant protein in a standard kinase assay with EC50 of 0.2 nM[1].

    In Vivo

    Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts[1].

    Clinical Trial
    Molecular Weight

    445.31

    Formula

    C₁₈H₁₆Cl₂F₂N₄OS

    CAS No.

    1047634-63-8

    SMILES

    O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[[email protected]@H](CC3=CC=C(F)C(F)=C3)CN

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Kinase Assay
    [1]

    The potency of compounds against Akt enzymes is measured. Since GSK2110183 and GSK2141795 are highly potent inhibitors of the 3 isoforms of Akt, the true potency (Ki) of the inhibitors is initially determined at low enzyme concentrations (0.1 nM Akt1, 0.7 nM Akt2, and 0.2 nM Akt3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSSFAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled Akt peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilized continuous real-time fluorescence detection of product formation using the Sox-Akt-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2) [1].

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

    Cell Assay
    [1]

    Cell lines are typically grown in RPMI 160 medium containing 10% FBS. Some cell lines are grown in media specified by the vendor. A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 µM. Cell growth is determined relative to untreated (DMSO) controls. EC50s are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application[1].

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

    Animal Administration
    [1]

    Mice[1]
    Tumors are initiated by injecting either cells (SKOV3, CAPAN-2 and HPAC) or a tumor fragments (BT474) subcutaneously into 6-8 week female athymic nude (SKOV3) and SCID (all others) mice. Once tumors reach between 120 and 300 mm3, mice are randomized according to tumor volume into groups of n = 7-10 mice per treatment. GSK2110183 (10, 30 or 100 mg/kg daily for 21 days) and GSK2141795 are administered daily at various doses by oral gavage. In combination experiments, GSK1120212 is also administered daily by oral gavage. Tumor volumes and body weight are measured twice weekly, tumor volume is measured with calipers and calculated.

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

    References
    • 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.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GSK2110183
    Cat. No.:
    HY-15966
    Quantity: