[CAS NO. 1276553-09-3] PF-4989216
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PRODUCTS SPECIFICATIONS [1276553-09-3]
Store
Catalog
SLK-S7675
Brand
Selleck
CAS
1276553-09-3
DESCRIPTION [1276553-09-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 380.4 |
| Molecular Formula | C18H13FN6OS |
| SMILES | N#CC1=C(N2CCOCC2)SC(C3=NC=NN3)=C1C4=CC=C(C#N)C=C4F |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
PF-4989216 is a potent and selective inhibitor with 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.
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