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

GSK2636771 

Cat. No.: HY-15245 Purity: 99.83%
COA 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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 117 In-stock
Solution
10 mM * 1 mL in DMSO USD 117 In-stock
Solid
5 mg USD 106 In-stock
10 mg USD 198 In-stock
50 mg USD 462 In-stock
100 mg USD 726 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

GSK2636771 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

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  • 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]

PI3Kβ

0.89 nM (Ki)

PI3Kβ

5.2 nM (IC50)

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].

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

GSK2636771 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

433.42

Appearance

Solid

Formula

C22H22F3N3O3
CAS No.
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 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (38.46 mM; ultrasonic and warming and heat to 60°C)

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 available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.83%

COA (255 KB) HNMR (259 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
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
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GSK2636771 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

GSK26367711372540-25-4GSK 2636771GSK-2636771PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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