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    PF-4989216
    PF-4989216

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0151
    CAS #: 1276553-09-3Purity ≥98%

    Description: PF-4989216 is a novel, potent, orally bioactive and selective small molecule inhibitor of PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity. It inhibits PI3K isoforms p110α, p110β, p110γ, p110δ, and VPS34 with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM, respectively. PF-4989216 inhibited PI3K downstream signaling and subsequently led to apoptosis induction, and inhibition in cell viability, transformation, and xenograft tumor growth in SCLCs harboring PIK3CA mutation. 

    References:  Clin Cancer Res. 2014 Feb 1;20(3):631-43.

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    Molecular Weight (MW)

    380.4

    Formula

    C18H13FN6OS

    CAS No.

    1276553-09-3

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 76 mg/mL (199.8 mM)

    Water:<1 mg/mL

    Ethanol: 7 mg/mL warming (18.4 mM)

    Solubility (In vivo)

    Suspended in 0.5% methylcellulose: 1mg/mL 

    Chemical Name / Synonym

    4-(4-cyano-2-fluorophenyl)-2-morpholino-5-(1H-1,2,4-triazol-3-yl)thiophene-3-carbonitrile; PF4989216; PF 4989216; PF-4989216


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    In VitroKinase Assay: PF-4989216 (Compound 10) has excellent PI3Kα Ki (0.6 nM), good cellular potency (S473 IC50=79 nM), and good selectivity against mTOR (mTOR Ki=1440 nM). PF-4989216 has PI3Kα Ki less than 1 nM and mTOR Ki more than 1 μM. PF-4989216 also has excellent selectivity over 40 other kinases, and no major CYP inhibitions are observed. Less than 30% inhibition is observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM.

    Cell Assay: 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. Cells NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells.

    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 VivoIn 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.
    Animal modelSCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors
    Formulation & DosageDissolved in  in 0.5% methylcellulose; 350 mg/kg; oral administration
    References[1] Walls M, et al. Clin Cancer Res. 2014, 20(3), 631-643.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-4989216

    PF-4989216 inhibited PI3K downstream signaling in SCLC cells. Clin Cancer Res. 2014, 20(3), 631-643.




    PF-4989216

    PF-4989216 inhibited PI3K phosphorylation signaling and induced antitumor activity in NCI-H1048 xenograft models. Clin Cancer Res. 2014, 20(3), 631-643.

    PF-4989216

    PF-4989216 inhibited PI3K phosphorylation signaling and induced antitumor activity in NCI-H1048 xenograft models. Clin Cancer Res. 2014, 20(3), 631-643.


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