A dual PI3K and mTOR inhibitor
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GNE-477

Item No. 27977

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[7-methyl-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-2-pyrimidinamine
CAS Number
1032754-81-6
Molecular Formula
C21H28N8O3S2
Formula Weight
504.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
NC1=NC=C(C=N1)C2=NC(N3CCOCC3)=C(SC(CN4CCN(S(C)(=O)=O)CC4)=C5C)C5=N2
InChi Code
InChI=1S/C21H28N8O3S2/c1-14-16(13-27-3-5-29(6-4-27)34(2,30)31)33-18-17(14)25-19(15-11-23-21(22)24-12-15)26-20(18)28-7-9-32-10-8-28/h11-12H,3-10,13H2,1-2H3,(H2,22,23,24)
InChi Key
AKKCGLXULFRAET-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $174

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    10 mg

    $329

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    25 mg

    $734

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    50 mg

    $1,120

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    Product Description

    GNE-477 is a dual inhibitor of PI3K (IC50 = 4 nM for PI3Kα) and mTOR (apparent Ki = 21 nM).1 It inhibits proliferation of MCF-7.1 cells with an EC50 value of 143 nM. It reduces tumor growth in a PC3-NCI tumor xenograft model when administered at doses ranging from 1 to 20 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heffron, T.P., Berry, M., Castanedo, G., et al. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. Bioorg. Med. Chem. Lett. 20(8), 2408-2411 (2010).