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.
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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.
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Choose Selective PI3K Inhibitors
|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.|
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.  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. 
|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. |
|In vitro||DMSO||28 mg/mL (64.6 mM)|
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Clinical Trial Information
|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|
|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|
|NCT02215096||Recruiting||Cancer||GlaxoSmithKline||November 13 2014||Phase 1|
|NCT01458067||Completed||Cancer||GlaxoSmithKline||November 10 2011||Phase 1|
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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