GSK2636771

For research use only.

Catalog No.S8002

13 publications

GSK2636771 Chemical Structure

CAS No. 1372540-25-4

GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.

Selleck's GSK2636771 has been cited by 13 publications

4 Customer Reviews

  • Cells were treated as indicated. Medium and drug were refreshed every 2 to 3 days, and protein lysates were analyzed as above.

    Clin Cancer Res, 2017, 23(11):2795-2805. GSK2636771 purchased from Selleck.

  • PI3K inhibitor GSK2636771 demonstrated to be effective on ALL-SIL cells, showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. GSK2636771 purchased from Selleck.

  • Effect of GSK2636771 on phosphorylation of Akt and integrin b1 in DU145 cells. Levels of p-integrin b1, integrin b1, p-Akt, Akt, and b-actin in DU145 cells treated with different concentrations of GSK2636771 were determined by Western blot analysis and quantified by ImageJ software.

    FASEB J, 2018, doi:10.1096/fj.201800183R. GSK2636771 purchased from Selleck.

  • Activity of LY2784544 and GSK2636771 at GPR39 and 11 additional understudied GPCRs.

    Mol Pharmacol, 2016, 90(6):726-737. GSK2636771 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.
Targets
PI3Kβ [1]
In vitro

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. [1] 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. [2]
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. [1]

Protocol

Cell Research:

[2]
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  • Cell lines: p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines.
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells 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.


    (Only for Reference)
Animal Research:

[3]
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  • Animal Models: Balb-c nude mice
  • Dosages: 100 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 28 mg/mL (64.6 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.42
Formula

C22H22F3N3O3
CAS No. 1372540-25-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=CC=C1C(F)(F)F)CN2C(=NC3=C(C=C(C=C32)N4CCOCC4)C(=O)O)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03131908 Active not recruiting Drug: GSK2636771|Drug: Pembrolizumab Melanoma and Other Malignant Neoplasms of Skin|Metastatic Melanoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|National Institutes of Health (NIH)|Merck Sharp & Dohme Corp.|GlaxoSmithKline July 17 2017 Phase 1|Phase 2
NCT02215096 Completed Drug: GSK2636771|Drug: Enzalutamide Neoplasms GlaxoSmithKline November 13 2014 Phase 1
NCT01458067 Completed Drug: GSK2636771 Cancer GlaxoSmithKline November 10 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID