An orally bioavailable PI3K inhibitor
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PF-4989216

Item No. 19308

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-cyano-2-fluorophenyl)-2-(4-morpholinyl)-5-(1H-1,2,4-triazol-5-yl)-3-thiophenecarbonitrile
CAS Number
1276553-09-3
Molecular Formula
C18H13FN6OS
Formula Weight
380.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 1 mg/ml
λmax
229, 309 nm
SMILES
FC(C=C(C#N)C=C1)=C1C2=C(C3=NN=CN3)SC(N4CCOCC4)=C2C#N
InChi Code
InChI=1S/C18H13FN6OS/c19-14-7-11(8-20)1-2-12(14)15-13(9-21)18(25-3-5-26-6-4-25)27-16(15)17-22-10-23-24-17/h1-2,7,10H,3-6H2,(H,22,23,24)
InChi Key
MUENOTXSRZEFJV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    10 mg

    $329

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    25 mg

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    Product Description

    PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC50s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively).1 It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking PI3K downstream signaling and inducing apoptosis.1 PF-4989216 prevents tumor growth of SCLC cells harboring PIK3CA mutation in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walls, M., Baxi, S.M., Mehta, P.P., et al. Targeting small cell lung cancer harboring PIK3CA mutation with a selective oral PI3K inhibitor PF-4989216. Clin. Cancer Res. 20(3), 631-643 (2014).