Omipalisib

SKU: orb1307306

Description

Omipalisib

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1086062-66-9
• MW: 505.5
• Purity: 99.80%
• Formula: C₂₅H₁₇F₂N₅O₃S
• SMILES: COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccnnc3)c2c1
• Target: Autophagy,mTOR,PI3K
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.96 mM);DMSO:50 mg/mL (98.91 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  p110δ:0.024 nM(Ki)|p110α-E542K:0.008 nM (Ki)|p110γ:0.06 nM(Ki)|p110α:0.019 nM(Ki)|p110α-E545K:0.008 nM (Ki)|mTORC1:0.18 nM(Ki)|mTORC2:0.3 nM (Ki)|p110β:0.13 nM(Ki)|p110α-H1047R:0.009 nM (Ki)
• In Vivo:
  In the BT474 human xenograft model, GSK2126458 (300 μg/kg) effectively inhibits tumor cell growth in a dose-dependent manner. Clinical trials have demonstrated that GSK2126458 possesses oral bioactivity in mice, rats, dogs, and monkeys, along with favorable blood clearance properties.
• In Vitro:
  GSK2126458 reduces the levels of pAKT-S473 in T47D cells (IC50=0.41 nM) and BT474 cells (IC50=0.18 nM), leading to cell cycle arrest at the G1 phase and inhibiting cell proliferation.
• Cell Research:
  BT474, HCC1954 and T-47D (human breast) are cultured in RPMI-1640 containing 10% fetal bovine serum at 37 °C in 5% CO2 incubator. Cells are split into T75 flask two to three days prior to assay set up at density which yields approximately 70-80% confluence at time of harvest for assay. Cells are harvested using 0.25% trypsin-EDTA. Cell counts are performed on cell suspension using Trypan Blue exclusion staining. Cells are then plated in 384 well black flat bottom polystyrene in 48 μL of culture media per well at 1,000 cells/well. All plates are placed at 5% CO2, 37 °C overnight and GSK2126458 is added the following day. One plate is treated with CellTiter-Glo for a day 0 (t=0) measurement and read as described below. GSK2126458 is prepared in clear bottom polypropylene 384 well plates with consecutive two fold dilutions. 4 μL of these dilutions are added to 105 μL culture media, after mixing the solution, 2 μL of these dilutions are added into each well of the cell plates. The final concentration of DMSO in all wells is 0.15%. Cells are incubated at 37 °C, 5% CO2 for 72 hours. Following 72 hours of incubation with GSK2126458 each plate is developed and read. CellTiter-Glo reagent is added to assay plates using a volume equivalent to the cell culture volume in the wells. Plates are shaken for approximately two minutes and incubated at room temperature for approximately 30 minutes and chemiluminescent signal is read on the Analyst GT reader. Results are expressed as a percent of the t=0 and plotted against the GSK2126458 concentration. Cell growth inhibition is determined for GSK2126458 by fitting the dose response with a 4 or 6 parameter curve fit using XLfit software and determining the concentration that inhibits 50% of the cell growth (gIC50) with the Y min as the t=0 and Y max as the DMSO control. Value from wells with no cells is subtracted from all samples for background correction.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | 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

GSK2126458, GSK-2126458, GSK 2126458, GSK 458, GSK458, GSK-458, Mammalian target of Rapamycin, inhibit, mTORC1, mTOR, Inhibitor, Omipalisib, Autophagy, Phosphoinositide 3-kinase, PI3K, p110α, p110δ, p110β, p110γ

Compound Identifiers

PubChem CID

25167777