Home PI3K/Akt/mTOR PI3K inhibitor PF-4989216 For research use only.

PF-4989216

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.

PF-4989216 Chemical Structure

PF-4989216 Chemical Structure

CAS No. 1276553-09-3

Purity & Quality Control

Batch: S767501 DMSO]76 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.86%
99.86

PF-4989216 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors
Dosages 350 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 380.4 Formula

C18H13FN6OS
CAS No. 1276553-09-3 SDF Download PF-4989216 SDF
Smiles C1COCCN1C2=C(C(=C(S2)C3=NC=NN3)C4=C(C=C(C=C4)C#N)F)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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