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    GSK2636771
    GSK2636771

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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 #: V0135
    CAS #: 1372540-25-4 Purity ≥98%

    Description: GSK2636771 is a novel, potent, selective and orally bioavailable inhibitor of PI3Kβ (phosphatidylinositol 3-kinase βwith potential anticancer activity. It inhibits PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity for PI3Kβ over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

    References:Clin Cancer Res. 2013 Jul 1;19(13):3533-44. 

    Related CAS: 2108806-07-9 (HCl salt); 1372540-91-4 (tris)

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    Molecular Weight (MW)

    433.42

    Formula

    C22H22F3N3O3

    CAS No.

    1372540-25-4 freebase

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 28 mg/mL (64.6 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    SMILES

    O=C(C1=C2C(N(CC3=CC=CC(C(F)(F)F)=C3C)C(C)=N2)=CC(N4CCOCC4)=C1)O

    Synonym/Chemical Name

    GSK2636771; GSK-2636771; GSK 2636771; 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid

     


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    In Vitro

    Kinase Assay: GSK2636771 is a potent, selective and oral inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

     

    Cell Assay: Cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value<0.05 is considered statistically significant.

    GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines.

    In Vivo

    GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice.

    Animal model

     Mice

    Formulation & Dosage

     100 mg/kg

    References

    Clin Cancer Res. 2013 Jul 1;19(13):3533-44.

     


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

    GSK2636771

    Clin Cancer Res. 2013, 19(13), 3533-3544.

    GSK2636771

    PI3K inhibition-induced Rb inactivation predicts subsequent apoptosis in PTEN-deficient, ER+ breast cancer cells.  2017 Jun 1;23(11):2795-2805.

    GSK2636771

    PI3K inhibition-induced Rb inactivation predicts subsequent apoptosis in PTEN-deficient, ER+ breast cancer cells.  2017 Jun 1;23(11):2795-2805.


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