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GSK2636771

Cat. No. M2050

All AbMole products are for research use only, cannot be used for human consumption.

GSK2636771 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 60  USD60 In stock
5mg USD 90  USD90 In stock
10mg USD 170  USD170 In stock
50mg USD 410  USD410 In stock
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Quality Control & Documentation
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.

Product Citations
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.
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 433.42
Formula C22H22F3N3O3
CAS Number 1372540-25-4
Solubility (25°C) DMSO 26 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Debashis Sarker, et al. A Phase I, Open-Label, Dose-Finding Study of GSK2636771, a PI3Kβ Inhibitor, Administered with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer

[2] Cristina Uribe-Alvarez, et al. Targeting effector pathways in RAC1 P29S-driven malignant melanoma

[3] Xin Su, et al. Development of a validated LC-MS/MS method for quantification of phosphoinositide 3 kinase inhibitor GSK2636771: Application to a pharmacokinetic study in rat plasma

[4] Ben-Yi Li, et al. PI3K/p110β-specific inhibitors in castration-resistant prostate cancer

[5] Joaquin Mateo, et al. A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors

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  Catalog
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Keywords: GSK2636771 supplier, PI3K, inhibitors, activators

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