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GSK2636771

Cat. No. M2050
GSK2636771 Structure
Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 350 In stock
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Quality Control
Biological Activity

GSK2636771 is a potent and selective, orally bioavailable inhibitor of phosphatidylinositol 3-kinase-beta (PI3Kβ) for the treatment of PTEN deficient tumors. GSK2636771 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 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK2636771 (100 mg/kg) do not increase glucose/insulin levels in mice. GSK2636771 is currently in Phase I/II trials.

Protocol
Cell Experiment
Cell lines EEC cell lines
Preparation method Cells were 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 24h, cells were treated with serial dilutions (100pM to 10μM) of PI3K and MAPK pathway inhibitors (Supplementary Methods, Supplementary Table 3). Cell viability was assessed after 72h of treatment by incubation with CellTiter Blue (Promega, Southampton, UK) for 1.5h.
Concentrations 100pM to 10μM
Incubation time 72h
Animal Experiment
Animal models 6- to 8-week-old female athymic nude mice BT474 tumor model
Formulation GSK2636771 was dissolved on 0.5% metilcellulose and 0.2% Tween 80.
Dosages 30mg/kg daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 433.42
Formula C22H22F3N3O3
CAS Number 1372540-25-4
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Cancer Cell (2015). Figure 3. GSK2636771 (Abmole)
Method Tumor growth assay
Cell Lines
Concentrations 30mg/kg per oral gavage daily
Incubation Time 21 days
Results Both BYL719 and GSK2636771, a structurally unrelated p110b inhibitor currently in clinical trials, slowed tumor growth but only the combination induced tumor shrinkage.
Rating
Source Cancer Cell (2015). Figure 3.GSK2636771 (Abmole)
Method Immunoblotting
Cell Lines BT-474, SKBR3 cell
Concentrations 1µM
Incubation Time 24 h
Results This led to the loss of p110b recruitment and the block of the rebound of AKT activation observed 24 hr after treatment with BYL719 alone.
Rating
Product Citations
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK2636771 supplier, PI3K, inhibitors

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