GSK2636771

Name: GSK2636771
Brand: Selleck Chemicals
SKU: S8002
Rating: 5 (12 reviews)

For research use only.

Catalog No.S8002

12 publications

Molecular Weight(MW): 433.42

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 12 publications

Front Oncol, 2020, 10;10:331

PubMed: 32211337 ( click the link to review the publication )

Small GTPases, 2020, 10.1080/21541248

PubMed: 32043900 ( click the link to review the publication )

Cancer Res, 2019, 79(7):1520-1534

PubMed: 30737233 ( click the link to review the publication )

Cell Signal, 2019, 53:122-131

PubMed: 30291869 ( click the link to review the publication )

J Exp Med, 2018, 215(1):159-175

PubMed: 29141866 ( click the link to review the publication )

Cancer, 2018, 124(18):3693-3705

PubMed: 30289966 ( click the link to review the publication )

FASEB J, 2018, 10.1096/fj.201800183R

PubMed: 29792732 ( click the link to review the publication )

PLoS One, 2018, 13(3):e0193921

PubMed: 29509781 ( click the link to review the publication )

Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2764

PubMed: 27903677 ( click the link to review the publication )

Mol Pharmacol, 2016, 90(6):726-737

PubMed: 27754899 ( click the link to review the publication )

Oncotarget, 2016, 10.18632/oncotarget.11205

PubMed: 27533080 ( click the link to review the publication )

Blood, 2015, 10.1182/blood-2014-11-610329

PubMed: 25957390 ( click the link to review the publication )

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)

References

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 Download GSK2636771 SDF

Molecular Weight	433.42
Formula	C₂₂H₂₂F₃N₃O₃
CAS No.	1372540-25-4
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CC1=NC2=C(C=C(C=C2[N]1CC3=CC=CC(=C3C)C(F)(F)F)N4CCOCC4)C(O)=O

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

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The Serial Dilution Calculator Equation

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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

Tel: +1-832-582-8158 Ext:3

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GSK2636771