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.

Size Price Stock Quantity  
10mM (1mL in DMSO) RMB 3863.69 In stock
RMB 2235.61 In stock
RMB 3029.66 In stock
RMB 8763.30 In stock
RMB 16298.10 In stock
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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.

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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