PF-4989216

SKU: orb1300330

Description

PF-4989216 is a potent and selective PI3K inhibitor, exhibiting IC50 values of 2 nM (p110α), 1 nM (p110δ), 65 nM (p110γ), 142 nM (p110β), and 110 nM (VPS34). This tool compound is used in biochemical and cellular assays to investigate PI3K signaling pathways in oncology and immunology research contexts.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1276553-09-3
• MW: 380.4
• Purity: 99.53%
• Formula: C₁₈H₁₃FN₆OS
• SMILES: Fc1cc(ccc1-c1c(sc(N2CCOCC2)c1C#N)-c1ncn[nH]1)C#N
• Target: PI3K,Apoptosis
• Solubility: Ethanol:7 mg/mL (18.4 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:71 mg/mL (186.65 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.26 mM)

Bioactivity

• Target IC50:
  p110δ:1 nM|PI3Kα:0.6 nM (Ki)|p110γ:65 nM|p110α:2 nM|mTOR:1440 nM (Ki)|VPS34:110 nM|p110β:142 nM
• In Vivo:
  In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity.
• In Vitro:
  PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis.
• Cell Research:
  SCLC cells are cultured (5,000 cells/well) in a 96-well microtiter plate at 37°C in 5% CO2 in supplier-recommended growth media and compounds are added to each well starting at 10 μM with a 3-fold serial dilution. At 72 hours after compound addition, CellTiter-Glo (CTG) Solution is added per the manufacturer's instructions. Luminescence is read on an Envision plate reader. All experiments are run in duplicate and have been repeated at least three times.(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

Apoptosis, Inhibitor, inhibit, p110β, p110γ, p110δ, p110α, PF 4989216, PF4989216, PF-4989216, Phosphoinositide 3-kinase, PI3K, Vps34

Compound Identifiers

PubChem CID

51033720