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GSK2636771
| Product Name | GSK2636771 |
| Price: | Inquiry |
| Catalog No.: | CN00153 |
| CAS No.: | 1372540-25-4 |
| Molecular Formula: | C22H22F3N3O3 |
| Molecular Weight: | 433.42 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | OC(=O)c1cc(cc2c1nc(n2Cc1cccc(c1C)C(F)(F)F)C)N1CCOCC1 |
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| Description | GSK2636771 is a potent, selective and oral 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. |
| Target | 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]. |
| 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]. |
| Cell Assay | 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, Temsirolimus, 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. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 641.3±55.0 °C at 760 mmHg |
| Flash Point | 341.7±31.5 °C |
| Exact Mass | 433.161316 |
| PSA | 67.59000 |
| LogP | 3.61 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |