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PF-4989216

Cat. No. M5335

All AbMole products are for research use only, cannot be used for human consumption.

PF-4989216 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 95 In stock
1mg USD 40 In stock
5mg USD 90 In stock
10mg USD 130 In stock
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Quality Control & Documentation
Biological Activity

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.

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.

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.

Chemical Information
Molecular Weight 380.4
Formula C18H13FN6OS
CAS Number 1276553-09-3
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wu CP, et al. Mol Pharm. Overexpression of ATP-binding cassette sub-family G member 2 confers resistance to phosphatidylinositol 3-kinase inhibitor PF-4989216 in cancer cells.

[2] Walls M, et al. Clin Cancer Res. Targeting small cell lung cancer harboring PIK3CA mutation with a selective oral PI3K inhibitor PF-4989216.

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-4989216 supplier, PI3K, inhibitors, activators

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



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