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

Afuresertib hydrochloride (Synonyms: GSK2110183 hydrochloride)

Cat. No.: HY-15727A Purity: 96.98%
Handling Instructions

Afuresertib hydrochloride (GSK 2110183 hydrochloride) 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 hydrochloride Chemical Structure

Afuresertib hydrochloride Chemical Structure

CAS No. : 1047645-82-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 114 In-stock
Estimated Time of Arrival: December 31
50 mg USD 324 In-stock
Estimated Time of Arrival: December 31
100 mg USD 564 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Afuresertib hydrochloride:

Top Publications Citing Use of Products

    Afuresertib hydrochloride 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 hydrochloride (GSK 2110183 hydrochloride) 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[2]

    Akt

     

    Akt1

    0.08 nM (Ki)

    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)

    ROCK

    100 nM (IC50)

    PKCθ

    510 nM (IC50)

    In Vitro

    Afuresertib (GSK 2110183) 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[2].

    Clinical Trial
    Molecular Weight

    463.78

    Formula

    C₁₈H₁₈Cl₃FN₄OS

    CAS No.

    1047645-82-8

    SMILES

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

    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 : ≥ 52 mg/mL (112.12 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1562 mL 10.7810 mL 21.5619 mL
    5 mM 0.4312 mL 2.1562 mL 4.3124 mL
    10 mM 0.2156 mL 1.0781 mL 2.1562 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
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    Afuresertib hydrochloride
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