- 貨號 Cat. No.
- S8002
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
GSK2636771
GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
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10mM/1mLIn DMSO |
USD 592 |
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5mg |
USD 340 |
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10mg |
USD 466 |
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50mg |
USD 1348 |
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200mg |
USD 3112 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a. |
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Targets |
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IC50 |
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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] |
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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] |
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Features |
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Protocol(Only for Reference)
Cell Assay: [2]
Cell lines |
p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines. |
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Concentrations |
~10 μM |
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Incubation Time |
72 hours |
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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. |
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1
References
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number |
Recruitment |
Conditions |
Sponsor
/Collaborators |
Start Date |
Phases |
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NCT01458067 |
Recruiting |
Cancer |
GlaxoSmithKline |
2011-11 |
Phase 1 |
Download GSK2636771 SDF
Molecular Weight (MW) |
433.42 |
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Formula |
C22H22F3N3O3
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CAS No. |
1372540-25-4 |
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Storage |
2 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
28 mg/mL (64 mM) |
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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)- |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.43342 |
4.3342 |
8.6684 |
13.0026 |
Customer Reviews (1)
Click to enlarge |
Rating |
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Source |
Dr Antonino Maria Spartà from University of Bologna.GSK2636771 purchased from Selleck |
Method |
MTT |
Cell Lines |
ALL-SIL cells |
Concentrations |
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Incubation Time |
48 h |
Results |
PI3K inhibitor GSK2636771 demonstrated to be effective on ALL-SIL cells, showed an IC50 in the lower micromolar range. |
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