A dual PI3Kα and mTOR inhibitor
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GNE-317

Item No. 27671

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[6-(3-methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-2-pyrimidinamine
CAS Number
1394076-92-6
Molecular Formula
C19H22N6O3S
Formula Weight
414.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
CC1=C(C2(OC)COC2)SC3=C(N4CCOCC4)N=C(C5=CN=C(N)N=C5)N=C31
InChi Code
InChI=1S/C19H22N6O3S/c1-11-13-14(29-15(11)19(26-2)9-28-10-19)17(25-3-5-27-6-4-25)24-16(23-13)12-7-21-18(20)22-8-12/h7-8H,3-6,9-10H2,1-2H3,(H2,20,21,22)
InChi Key
XOZLHJMDLKDZAL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $43

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    10 mg

    $77

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    25 mg

    $183

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    50 mg

    $323

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    Product Description

    GNE-317 is a dual inhibitor of PI3Kα and the mammalian target of rapamycin (mTOR; apparent Kis = 2 and 9 nM, respectively).1 It inhibits the proliferation of PC3 prostate cancer and A172 glioblastoma cells with EC50 values of 132 and 240 nM, respectively. GNE-317 (10-40 mg/kg) reduces tumor growth in a U87MG/M glioblastoma mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heffron, T.P., Salphati, L., Alicke, B., et al. The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. J. Med. Chem. 55(18), 8007-8020 (2012).