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    GNE-317
    GNE-317

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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 #: V0146
    CAS #: 1394076-92-6Purity ≥98%

    Description: GNE-317, an oxetane analog of GDC-0980,  is a novel, potent, and selective PI3K/mTOR dual inhibitor with excellent BBB (blood-brain barrier) penetrating ability. It inhibits PI3K α-isoform with a Ki of 2 nM. and has potential anticancer activity. GNE-317 is not a substrate of the efflux pumps such as P-gp or BCRP which cuases drug resostance.

    References:  Clin Cancer Res. 2012 Nov 15;18(22):6239-48; Drug Metab Dispos. 2014 Jul;42(7):1110-6. 

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    Molecular Weight (MW)

    414.48

    Formula

    C19H22N6O3S

    CAS No.

    1394076-92-6

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 47 mg/mL warming (113.4 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Synonym

    GNE317; GNE 317; GNE-317

    Chemical Name

    5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine


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    In VitroKinase Assay: GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).

    Cell Assay: GNE-317 is not a substrate of P-gp or BCRP transporter in transfected Madin-Darby canine kidney (MDCK) cells. Binding of GNE-317 to plasma proteins exhibits a free fraction of 14.9 % in mouse plasma, and binding to brain tissues is higher, with a free fraction of 5.4%. GNE-317 shows cytostasis but no cell death to U87 cells.

    In VivoGNE-317 (40 mg/kg, p.o.) markedly inhibits the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 (40 mg/kg, p.o.) is efficacious in the U87 and GS2 orthotopic models, achieving tumor growth inhibition of 90% and 50%, respectively. In the GBM10 tumor model, GNE-317 (30 mg/kg, p.o.; 40 mg/kg the first 2 weeks) extends the survival of mice from a median of 55.5 to 75 days.
    Animal modelU87 and GS2 orthotopic tumor-bearing mice.
    Formulation & DosageDissolved in 0.5% methylcellulose/0.2%Tween 80; 40 mg/kg; Oral administration
    References[1] Salphati L, et al. Clin Cancer Res. 2012, 18(22):6239-6248.


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

    GNE-317

    GNE-317
    GNE-317
    A, chemical structure of GNE-317. B, plasma concentration-time profile and brain concentrations of GNE-317 following PO administration (50 mg/kg) to CD-1 mice. C, Western blotting of mouse brains probed with antibodies against pAkt, total Akt, pS6, total S6, p4EBP1, total 4EBP1 and actin. D, quantitation of pAkt/total Akt, p4EBP1/total 4EBP1 and pS6/total S6 at 1 and 6 hours postdose in CD-1 mice. B and D.

    Clin Cancer Res. 2012, 18(22):6239-6248

    Efficacy in orthotopic models of glioblastoma. A, efficacy of GNE-317, GDC-0941, and GDC-0980 in GS2 neurosphere tumor model following treatment with GNE-317 at 40 mg/kg, GDC-0941 at 250 mg/kg or GDC-0980 at 10 mg/kg, daily for 6 weeks. B, GS2 brain tumor volume in control mice and mice treated with GNE-317, GDC-0941, or GDC-0980 for 6 weeks. Results are presented as the mean ± S.E. of 10 animals. C, efficacy of GNE-317 and GDC-0941 in U87 glioblastoma tumor model following treatment with GNE-317 at 40 mg/kg or GDC-0941 at 250 mg/kg, daily for 3 weeks. D, U87 brain tumor volume in control mice and mice treated with GNE-317 or GDC-0941 for 3 weeks.

    Immunohistochemical analysis of GS2 (A to C) and U87 (D to F) tumor-bearing brain sections from untreated mice and mice dosed with GDC-0941 (250 mg/kg) or GNE-317 (40 mg/kg). Sections were probed for the PI3K pathway marker pAkt. A and D, tumors from untreated animals; B and D, tumors from animal treated with GDC-0941; C and F, tumors from animals treated with GNE-317.


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