GSK2636771

Catalog No.S8002
1 Reviews

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.

Price Stock Quantity  
In DMSO USD 470 In stock
USD 270 In stock
USD 370 In stock
USD 1070 In stock
USD 2470 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

GSK2636771 Chemical Structure

GSK2636771 Chemical Structure
Molecular Weight: 433.42

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

PI3K Inhibitors with Unique Features

  • Pan PI3K Inhibitor

    LY294002 Pan-PI3Kα/δ/β inhibitor, IC50=0.5 μM/0.57 μM/0.97 μM.

  • Most Potent PI3K Inhibitor

    IPI-145 (INK1197) PI3K δ, IC50=1 nM.

  • Inhibitor in Clinical Trial

    Hexestrol Phase II for Advanced Breast Cancer.

  • Newest PI3K Inhibitor

    VS-5584 (SB2343) Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

Product Information

  • Compare PI3K Inhibitors
    Compare PI3K Inhibitors
  • Research Area

Product Description

Biological Activity

Description GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
Targets
IC50
In vitro GSK-2636771 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. [1] GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. [2]
In vivo GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice. [1]
Features

Protocol(Only for Reference)

Cell Assay: [2]

Cell lines p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines.
Concentrations ~10 μM
Incubation Time 72 hours
Method 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 (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). 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 (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant.
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01458067 Recruiting Cancer GlaxoSmithKline 2011-11 Phase 1

Chemical Information

Download GSK2636771 SDF
Molecular Weight (MW) 433.42
Formula

C22H22F3N3O3

CAS No. 1372540-25-4
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 28 mg/mL (64 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.43342 4.3342 8.6684 13.0026

Research Area

Customer Reviews (1)


Click to enlarge
Rating
Source Dr Antonino Maria Spartà from University of Bologna. GSK2636771 purchased from Selleck
Method MTT
Cell Lines ALL-SIL cells
Concentrations
Incubation Time 48 h
Results PI3K inhibitor GSK2636771 demonstrated to be effective on ALL-SIL cells, showed an IC50 in the lower micromolar range.

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PI3K Inhibitors

  • IPI-145 (INK1197)

    IPI-145 (INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM, highly selective for PI3K δ/γ than other protein kinases. Phase 2.

  • GSK2636771

    GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.

  • GDC-0032

    GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

    Features:A beta isoform-sparing PI3K inhibitor.

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1. Phase 1/2.

  • GDC-0941

    GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

  • LY294002

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Phase 3.

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 1/2.

  • PI-103

    PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

    Features:The first potent, synthetic mTOR inhibitor.

  • TGX-221

    TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM, 1000-fold more selective for p110β than p110α.

Recently Viewed Items

Tags: buy GSK2636771 | GSK2636771 supplier | purchase GSK2636771 | GSK2636771 cost | GSK2636771 manufacturer | order GSK2636771 | GSK2636771 distributor
Contact Us