GSK2636771

Catalog No.S8002

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.

Cited by 8 Publications

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

PubMed: 25957390 ( 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 )

Cell Signal, 2019, 53:122-131

PubMed: 30291869 ( 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 )

Oncotarget, 2016, 10.18632/oncotarget.11205

PubMed: 27533080 ( 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.

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.

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.

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]	+ Expand 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]	+ Expand Animal Models: Balb-c nude mice Formulation: CMC/Tween Dosages: 100 mg/kg Administration: oral administration (Only for Reference)

Cell Research:

^[2]

+ Expand

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]

+ Expand

Animal Models: Balb-c nude mice
Formulation: CMC/Tween
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

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03131908	Recruiting	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
NCT03131908	Recruiting	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
NCT02615730	Recruiting	Advanced Gastric Adenocarcinoma	Yonsei University	February 2016	Phase 1\|Phase 2
NCT02615730	Recruiting	Advanced Gastric Adenocarcinoma	Yonsei University	February 2016	Phase 1\|Phase 2
NCT02465060	Recruiting	Advanced Malignant Solid Neoplasm\|Bladder Carcinoma\|Breast Carcinoma\|Cervical Carcinoma\|Colon Carcinoma\|Colorectal Carcinoma\|Endometrial Carcinoma\|Esophageal Carcinoma\|Gastric Carcinoma\|Glioma\|Head and Neck Carcinoma\|Kidney Carcinoma\|Liver and Intrahepatic Bile Duct Carcinoma\|Lung Carcinoma\|Lymphoma\|Malignant Uterine Neoplasm\|Melanoma\|Ovarian Carcinoma\|Pancreatic Carcinoma\|Plasma Cell Myeloma\|Prostate Carcinoma\|Rectal Carcinoma\|Recurrent Bladder Carcinoma\|Recurrent Breast Carcinoma\|Recurrent Cervical Carcinoma\|Recurrent Colon Carcinoma\|Recurrent Colorectal Carcinoma\|Recurrent Esophageal Carcinoma\|Recurrent Gastric Carcinoma\|Recurrent Glioma\|Recurrent Head and Neck Carcinoma\|Recurrent Liver Carcinoma\|Recurrent Lung Carcinoma\|Recurrent Lymphoma\|Recurrent Malignant Solid Neoplasm\|Recurrent Melanoma\|Recurrent Ovarian Carcinoma\|Recurrent Pancreatic Carcinoma\|Recurrent Plasma Cell Myeloma\|Recurrent Prostate Carcinoma\|Recurrent Rectal Carcinoma\|Recurrent Skin Carcinoma\|Recurrent Thyroid Gland Carcinoma\|Recurrent Uterine Corpus Carcinoma\|Refractory Lymphoma\|Refractory Malignant Solid Neoplasm\|Refractory Plasma Cell Myeloma\|Skin Carcinoma\|Thyroid Gland Carcinoma\|Uterine Corpus Cancer	National Cancer Institute (NCI)	August 12 2015	Phase 2
NCT02465060	Recruiting	Advanced Malignant Solid Neoplasm\|Bladder Carcinoma\|Breast Carcinoma\|Cervical Carcinoma\|Colon Carcinoma\|Colorectal Carcinoma\|Endometrial Carcinoma\|Esophageal Carcinoma\|Gastric Carcinoma\|Glioma\|Head and Neck Carcinoma\|Kidney Carcinoma\|Liver and Intrahepatic Bile Duct Carcinoma\|Lung Carcinoma\|Lymphoma\|Malignant Uterine Neoplasm\|Melanoma\|Ovarian Carcinoma\|Pancreatic Carcinoma\|Plasma Cell Myeloma\|Prostate Carcinoma\|Rectal Carcinoma\|Recurrent Bladder Carcinoma\|Recurrent Breast Carcinoma\|Recurrent Cervical Carcinoma\|Recurrent Colon Carcinoma\|Recurrent Colorectal Carcinoma\|Recurrent Esophageal Carcinoma\|Recurrent Gastric Carcinoma\|Recurrent Glioma\|Recurrent Head and Neck Carcinoma\|Recurrent Liver Carcinoma\|Recurrent Lung Carcinoma\|Recurrent Lymphoma\|Recurrent Malignant Solid Neoplasm\|Recurrent Melanoma\|Recurrent Ovarian Carcinoma\|Recurrent Pancreatic Carcinoma\|Recurrent Plasma Cell Myeloma\|Recurrent Prostate Carcinoma\|Recurrent Rectal Carcinoma\|Recurrent Skin Carcinoma\|Recurrent Thyroid Gland Carcinoma\|Recurrent Uterine Corpus Carcinoma\|Refractory Lymphoma\|Refractory Malignant Solid Neoplasm\|Refractory Plasma Cell Myeloma\|Skin Carcinoma\|Thyroid Gland Carcinoma\|Uterine Corpus Cancer	National Cancer Institute (NCI)	August 12 2015	Phase 2

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.

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GSK2636771

Cited by 8 Publications

4 Customer Reviews

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download GSK2636771 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Total Molecular Weight: g/mol

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products4

Choose Your Country or Region

By Signaling Pathways

By product type

GSK2636771

Cited by 8 Publications

4 Customer Reviews

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download GSK2636771 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products4

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)