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GSK1059615
| Product Name | GSK1059615 |
| Price: | Inquiry |
| Catalog No.: | CN00107 |
| CAS No.: | 958852-01-2 |
| Molecular Formula: | C18H11N3O2S |
| Molecular Weight: | 333.36 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C1NC(=O)/C(=C/c2ccc3c(c2)c(ccn3)c2ccncc2)/S1 |
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| Description | GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. |
| Target | PI3Kα:0.4 nM (IC50) PI3Kβ:0.6 nM (IC50) PI3Kδ:5 nM (IC50) PI3Kγ:2 nM (IC50) mTOR:12 nM (IC50) |
| In Vitro | GSK1059615 inhibits PI3Kα, β, γ and δ, with Ki of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively[1]. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM[2]. |
| In Vivo | GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells[1]. |
| Cell Assay | Cells are plate at a density of 1×104 cells per well in clear flat-bottomed 96-well plates and incubated overnight. Then, GSK1059615 is added and the plates are incubated for 30 min. At the end of incubation, media is aspirated from the plates, and the plate is wash once with cold PBS. 80 μL MSD Lysis buffer is added into each well and the plates are incubated on a shaker at 4°C for at least 30 min. For Akt duplex assay, plates are washed with 200 μL/well wash buffer for 4 times and tapped on paper towel to blot. Then, 60 μL lysates is added to each well and the plates are incubated on shaker at room temperature for 1 hour. After another 4 times washing, antibody is added (25 μL per well) and the plates are incubated on shaker for 1 hour and washed again. Finally, Read Buffer is added (150 μL per well) and the plates are read immediately. IC50 values are then obtained. |
| Density | 1.4±0.1 g/cm3 |
| Exact Mass | 333.057190 |
| PSA | 97.25000 |
| LogP | 1.78 |
| Storage condition | Store at +4°C |