A PI3K p110α inhibitor
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PI3-Kinase α Inhibitor 2

Item No. 10010177

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl-phenol
CAS Number
371943-05-4
Synonyms
  • PI3Kα Inhibitor 2
  • Phosphatidylinositol 3-Kinase α Inhibitor 2
Molecular Formula
C16H15N3O2S
Formula Weight
313.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2) (1:3): 0.25mg/mlDMSO: 25 mg/mlEthanol: 1 mg/ml
λmax
255, 299 nm
SMILES
Oc1cccc(c1)c1nc2ccsc2c(n1)N1CCOCC1
InChi Code
InChI=1S/C16H15N3O2S/c20-12-3-1-2-11(10-12)15-17-13-4-9-22-14(13)16(18-15)19-5-7-21-8-6-19/h1-4,9-10,20H,5-8H2
InChi Key
XXLAEKOWCYJOKK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $31

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    1 mg

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    5 mg

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    Product Description

    PI3-Kinase α (PI3Kα) inhibitor 2 is an inhibitor of PI3K p110α (IC50 = 2 nM in an enzyme assay).1 It is selective for p110α over p110β, p110γ, and PI3K C2β (IC50s = 16, 660, and 220 nM, respectively). It also inhibits mammalian target of rapamycin (mTOR; IC50 = 49 nM).2 PI3Kα inhibitor 2 inhibits proliferation in A375 melanoma cells with an IC50 value of 0.58 μM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hayakawa, M., Kaizawa, H., Moritomo, H., et al. Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors. Bioorg. Med. Chem. 14(20), 6847-6858 (2006).

    2. Verheijen, J.C., Yu, K., Toral-Barza, L., et al. Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. Bioorg. Med. Chem. Lett. 20(1), 375-379 (2010).

    Product Citations

    Sun, Y.-Y., Lin, S.-H., Lin, H.-C., et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. PLoS One 8(7), e69019 (2013).