GSK2636771

SKU: orb1306552

Description

GSK2636771 is a potent, selective, and orally bioavailable inhibitor of PI3Kβ. It is used in research for studying various cancers, including lymphoma and solid tumors, and has been evaluated in both in vitro assays and in vivo xenograft models for advanced malignancies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1372540-25-4
• MW: 433.42
• Purity: 99.97%
• Formula: C₂₂H₂₂F₃N₃O₃
• SMILES: Cc1nc2c(cc(cc2n1Cc1cccc(c1C)C(F)(F)F)N1CCOCC1)C(O)=O
• Target: PI3K
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:9 mg/mL (20.77 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3Kβ:5.2 nM|PI3Kβ:0.89 nM (Ki)
• 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.
• 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).
• 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)

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

Phosphoinositide 3-kinase, PI3K, PI3Kβ, inhibit, Inhibitor, GSK2636771, GSK-2636771, GSK 2636771

Compound Identifiers

PubChem CID

56949517