For research use only.
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.
Selleck's GSK2636771 has been cited by 12 publications
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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.
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.
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|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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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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