PF-4989216

Catalog No.S7675

PF-4989216 Chemical Structure

Molecular Weight(MW): 380.4

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

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Biological Activity

Description PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
Targets
p110δ [1]
(Cell-free assay)
p110α [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
1 nM 2 nM 65 nM
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. [1]

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. [1]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells.
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors
  • Formulation: Suspended in 0.5% methylcellulose
  • Dosages: 350 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.78 mM)
Ethanol 7 mg/mL warmed (18.4 mM)
Water Insoluble
In vivo Add solvents individually and in order:
Suspended in 0.5% methylcellulose
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.4
Formula

C18H13FN6OS

CAS No. 1276553-09-3
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID