1. PI3K/Akt/mTOR
    TGF-beta/Smad
    Epigenetics
    Stem Cell/Wnt
    Cytoskeleton
    Cell Cycle/DNA Damage
  2. Akt
    PKC
    ROCK
  3. Afuresertib

Afuresertib (Synonyms: GSK2110183)

Cat. No.: HY-15727 Purity: 99.23%
Handling Instructions

Afuresertib (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.

Afuresertib Chemical Structure

Afuresertib Chemical Structure

CAS No. : 1047644-62-1

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10 mM * 1  mL in DMSO USD 92 In-stock
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10 mg USD 114 In-stock
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50 mg USD 324 In-stock
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100 mg USD 564 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Afuresertib:

Top Publications Citing Use of Products

    Afuresertib purchased from MCE. Usage Cited in: J Physiol. 2017 Jul 1;595(13):4207-4225.

    Effects of pharmacological inhibitors on AngII-mediated activation of L-type Ca2+ channels in NVCMs. NVCMs are treated with vehicle, Erlotinib, H-89, Afuresertib (1 μM), Gö6983, CID755673, KN-93, SCH772984, Bosutinib or Quinalizarin for 30 min before treatment of AngII.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Afuresertib (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[1][2].

    IC50 & Target[1]

    Akt2

    2 nM (Ki)

    Akt3

    2.6 nM (Ki)

    Akt1 E17K mutant

    0.2 nM (IC50)

    PKCη

    210 nM (IC50)

    PKC-βI

    430 nM (IC50)

    PKCθ

    510 nM (IC50)

    ROCK

    100 nM (IC50)

    In Vitro

    Afuresertib (GSK2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response[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

    427.32

    Formula

    C₁₈H₁₇Cl₂FN₄OS

    CAS No.

    1047644-62-1

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 40 mg/mL (93.61 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3402 mL 11.7008 mL 23.4017 mL
    5 mM 0.4680 mL 2.3402 mL 4.6803 mL
    10 mM 0.2340 mL 1.1701 mL 2.3402 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 (5.85 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    MPM cells are seeded in 96-well plates (cell density, 2.5×103 cells/well) and are incubated for 24 h at 37°C. Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g., Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer[1].

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

    References

    Purity: 99.23%

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    Keywords:

    AfuresertibGSK2110183GSK 2110183GSK-2110183AktPKCROCKPKBProtein kinase BProtein kinase CRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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