Home PI3K/Akt/mTOR PI3K inhibitor PF-4989216

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PF-4989216 PI3K inhibitor

Cat.No.S7675

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 PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 380.4

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 76 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 380.4 Formula

C18H13FN6OS

 Storage (From the date of receipt)
CAS No. 1276553-09-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1COCCN1C2=C(C(=C(S2)C3=NC=NN3)C4=C(C=C(C=C4)C#N)F)C#N

Mechanism of Action

Targets/IC50/Ki
p110δ
(Cell-free assay)
1 nM
p110α
(Cell-free assay)
2 nM
p110γ
(Cell-free assay)
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. This compound, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, it induces BIM-mediated apoptosis.
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.
References

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