GSK1059615

SKU: orb1305601

Description

GSK1059615 is a research compound that has been investigated in clinical trials for various cancers, including lymphoma, solid tumors, endometrial cancer, and metastatic breast cancer. It functions as a potent and selective PI3K inhibitor, with studies demonstrating its activity in both in vitro cellular assays and in vivo tumor models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 958852-01-2
• MW: 333.36
• Purity: 99.30%
• Formula: C₁₈H₁₁N₃O₂S
• SMILES: O=C1NC(=O)\C(S1)=C\c1ccc2nccc(-c3ccncc3)c2c1
• Target: mTOR,Apoptosis,PI3K
• Solubility: DMSO:5 mg/mL (15 mM)

Bioactivity

• Target IC50:
  mTOR:12 nM|PI3Kγ:5 nM|PI3Kβ:0.6 nM|PI3Kα:0.4 nM|PI3Kδ:2 nM
• In Vivo:
  GSK1059615 inhibited the PI3K pathway and induced cell arrest in G1 phase, and apoptosis was observed.GSK1059615 inhibited PI3K and decreased intracellular AKT phosphorylation at Ser473 in T47D and BT474 cancer cells with an IC50 of 40 nM.GSK1059615 also inhibited mTOR with an IC50 of 12 nM.
• In Vitro:
  GSK1059615 (25 mg/kg) effectively inhibited tumor growth in a xenograft mouse model of BT474 or HCC1954 breast cancer cells.
• Cell Research:
  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.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, mTOR, GSK1059615, GSK-1059615, GSK 1059615, Inhibitor, Mammalian target of Rapamycin, Apoptosis, PI3Kγ, PI3Kβ, PI3Kδ, PI3Kα, PI3K, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

23582824