GSK2636771

Catalog No.S8002

For research use only.

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.

GSK2636771 Chemical Structure

CAS No. 1372540-25-4

Selleck's GSK2636771 has been cited by 14 publications

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 (from reference)

Cell Research:

[2]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC=C1C(F)(F)F)CN2C(=NC3=C(C=C(C=C32)N4CCOCC4)C(=O)O)C

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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