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GSK2636771

Catalog No.
B2186
PIK3 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$90.00
In stock
5mg
$76.00
In stock
10mg
$143.00
In stock
50mg
$333.00
In stock
100mg
$523.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GSK2636771 is a p110β isoform-specific inhibitor of PIK3 with SF50 more than 1 μM [1].
PI3K (phosphatidylinositol 3-kinase) has 4 catalytic subunits: p110α, β, δ, γ,and δ. PI3K /AKT and related pathways play important roles in cellular growth and survival via internalizing the effects of external growth factors and membrane tyrosine kinases. [2, 3]. Many studies have shown that PI3K is over activated in a variety of cancer cells and inhibition of this pathway have been focused for cancer patients [4].
GSK2636771 is a selective PI3K inhibitor with targeting p110βand has different with the reported GDC-0941 which inhibits all class I PI3K isoforms. In breast cancer cell lines, treatment with GSK2636771 could significantly decrease the phosphorylation of AKT thus inhibits the cell viability. For EEC cell lines with PTEN-mutant, p110β inhibitor GSK2636771 should only combine with p110α selective inhibitor A66 to decrease cell viability [1].
References:
1.Weigelt, B., et al., PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res, 2013. 19(13): p. 3533-44.
2.Costa, C., et al., Measurement of PIP Levels Reveals an Unexpected Role for p110beta in Early Adaptive Responses to p110alpha-Specific Inhibitors in Luminal Breast Cancer. Cancer Cell, 2014. 24(14): p. 00458-9.
3.Schwartz, S., et al., Feedback Suppression of PI3Kalpha Signaling in PTEN-Mutated Tumors Is Relieved by Selective Inhibition of PI3Kbeta. Cancer Cell, 2014. 24(14): p. 00459-0.
4.Slomovitz, B.M. and R.L. Coleman, The PI3K/AKT/mTOR pathway as a therapeutic target in endometrial cancer. Clin Cancer Res, 2012. 18(21): p. 5856-64.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt433.42
Cas No.1372540-25-4
FormulaC22H22F3N3O3
Solubilityinsoluble in H2O; insoluble in EtOH; ≥10.83 mg/mL in DMSO
Chemical Name2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1=C(C=CC=C1C(F)(F)F)CN2C(=NC3=C2C=C(C=C3C(=O)O)N4CCOCC4)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

The human endometrioid endometrial cancer (EEC) cell lines harboring PIK3CA and PTEN mutations

Preparation method

The solubility of this compound in DMSO is >10.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1or 10μM for 72h

Applications

GSK2636771 significantly decreased cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and led to a marked decrease of AKT phosphorylation.

Animal experiment [2]:

Animal models

Balb-c nude mice

Dosage form

Oral, 100 mg/kg

Application

GSK-2636771 decreased phosphorylated protein kinase Akt (Ser473) levels in these xenograft models, and it did not increase glucose/insulin levels in mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Weigelt B., et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013, 19(13), 3533-3544.

[2]. Macauley D,, et al. Drugs Fut, 2012, 37(6), 451.

Quality Control

Chemical structure

GSK2636771