Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 36.00 | |
2 mg | In stock | $ 52.00 | |
5 mg | In stock | $ 81.00 | |
10 mg | In stock | $ 153.00 | |
25 mg | In stock | $ 267.00 | |
50 mg | In stock | $ 378.00 | |
100 mg | In stock | $ 576.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 81.00 |
Description | GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm. |
Targets&IC50 | PI3Kβ:5.2 nM |
In vitro | In mice, GSK-2636771 (at a dosage of 100 mg/kg) does not elevate glucose/insulin levels. In xenograft tumor models, GSK-2636771 decreases the levels of phosphorylated protein kinase Akt (Ser473). |
In vivo | In PTEN-deficient cell lines, GSK-2636771 exhibits specific inhibitory activity, with EC50 values of 36 nM in human prostate cancer PC-3 and 72 nM in breast cancer HCC70. |
Cell Research | 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. (Only for Reference) |
Synonyms | GSK 2636771, GSK-2636771 |
Molecular Weight | 433.42 |
Formula | C22H22F3N3O3 |
CAS No. | 1372540-25-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 27 mg/mL (62.3 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GSK2636771 1372540-25-4 PI3K/Akt/mTOR signaling PI3K Inhibitor Phosphoinositide 3-kinase GSK 2636771 inhibit GSK-2636771 inhibitor