1. PI3K/Akt/mTOR
  2. Akt

Afuresertib (Synonyms: GSK2110183C)

Cat. No.: HY-15727 Purity: 98.95%
Handling Instructions

Afuresertib is a potent and ATP-competitive specific Akt inhibitor.

For research use only. We do not sell to patients.
Afuresertib Chemical Structure

Afuresertib Chemical Structure

CAS No. : 1047644-62-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 114 In-stock
50 mg USD 324 In-stock
100 mg USD 564 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Afuresertib:

    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.

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Afuresertib is a potent and ATP-competitive specific Akt inhibitor.

    IC50 & Target[1]

    Akt

     

    In Vitro

    Afuresertib 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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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.
    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
    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

    Storage

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 40 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    Afuresertib
    Cat. No.:
    HY-15727
    Quantity: