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    Afuresertib (GSK-2110183)
    Afuresertib (GSK-2110183)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0169
    CAS #: 1047644-62-1Purity ≥98%

    Description: Afuresertib (also named as GSK2110183C) is a potent, orally bioavailable and ATP-competitive Akt inhibitor with potential anticancer activity. It inhibits Akt1, Akt2, and Akt3 with Kis of 0.08 nM, 2 nM, and 2.6 nM, respectively. As an inhibitor of the serine/threonine protein kinase Akt (protein kinase B), Afuresertib has potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. 

    References:  Cancer Chemother Pharmacol. 2015 Jan;75(1):183-9; Blood. 2014 Oct 2;124(14):2162-3. 

    Related CAS: 1047645-82-8 (Afuresertib HCl / GSK2110183B); 1047634-63-8 (GSK2110183); 2070009-64-0 (Afuresertib-F; GSK-2110183-analog HCl)  

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    Molecular Weight (MW)427.32
    FormulaC18H17Cl2FN4OS
    CAS No.1047644-62-1(Afuresertib / GSK2110183C)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[[email protected]@H](CC3=CC=CC(F)=C3)CN
    Synonyms/Chemical NameGSK2110183C; GSK-2110183C; GSK 2110183C; GSK2110183 C; GSK2110183-C; GSK2110183C; N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide


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    In Vitro

    Kinase Assay: The true potency (Ki*) of the inhibitor 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-KKGGRARTSS-FAEPG-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 utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2).

     

    Cell Assay: 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. EC50’s are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application. Cells used: Hematological cell lines and solid tumor cell lines

    Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.

    In Vivo

    Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively

    Animal model

    Female athymic nude and SCID mice bearing SKOV3 or BT474 tumors

    Formulation & Dosage

    Dissolved in 20% polyethylene glycol (PEG) 400/1% DMSO; 25, 50, 100 mg/kg; p.o.

    References

    [1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Afuresertib (GSK2110183)

    Effect of GSK2110183 on AKT signaling and growth inhibition in human cancer cell lines. PLoS One, 2014, 9(6):e100880.



    Afuresertib (GSK2110183)

    The impact of GSK2110183 and GSK2141795 on glucose homeostasis in vivo.

    Afuresertib (GSK2110183)

    Combination anti-tumor effect of AKT and MEK inhibitors in mouse models of pancreatic cancer.


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