1. PI3K/Akt/mTOR
  2. PI3K
  3. GSK2636771

GSK2636771 

Cat. No.: HY-15245 Purity: 99.86%
Handling Instructions

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

For research use only. We do not sell to patients.

GSK2636771 Chemical Structure

GSK2636771 Chemical Structure

CAS No. : 1372540-25-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

IC50 & Target[1]

p110β

 

In Vitro

GSK2636771 treatment causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

433.42

Formula

C₂₂H₂₂F₃N₃O₃

CAS No.

1372540-25-4

SMILES

CC1=NC2=C(C(O)=O)C=C(C=C2N1CC3=CC=CC(C(F)(F)F)=C3C)N4CCOCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (57.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3072 mL 11.5362 mL 23.0723 mL
5 mM 0.4614 mL 2.3072 mL 4.6145 mL
10 mM 0.2307 mL 1.1536 mL 2.3072 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.77 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Cells are 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 24 h, cells are treated with serial dilutions (100 pM to 10 µM) of the PI3K pathway inhibitors GDC-0941, A66, TGX-221, GSK2636771, AZD6482, CCI-779, AZD8055, PF-04691502, and of the MAPK pathway inhibitors AZD6244, PD0325901, AZD628, and PLX4032. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration required for survival of 50% of cells relative to untreated cells is determined using GraphPad Prism version 5.0 d. Cell lines that fail to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (10 µM). At least three independent experiments in triplicate per cell line/targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test, and a two-tailed P value.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.86%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK2636771GSK 2636771GSK-2636771PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK2636771
Cat. No.:
HY-15245
Quantity:
MCE Japan Authorized Agent: