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    LY2584702
    LY2584702

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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 #: V0240
    CAS #: 1082949-67-4Purity ≥98%

    Description: LY2584702 is a novel, selective, orally bioavailable, and ATP-competitive inhibitor of p70S6K (ribosomal p70 S6 kinase) with potential antitumor activity. It inhibits p70S6K with an IC50 of 4 nM. LY2584702 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo by inhibiting ribosomal protein S6 Kinase (p70S6K), and preventing phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation.  

    References:Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.

    Related CAS: 1082949-68-5 (tosylate); 1082948-81-9 (HCl); 1082949-67-4 (free base) 

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    Molecular Weight (MW)

    445.42

    Formula

    C21H19F4N7

    CAS No.

    1082949-67-4  (free base); 

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 1 mg/mL (2.2 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    SMILES

     CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3

    Synonyms

     LYS6K2; LY 2584702; LY-2584702; LY2584702; LYS 6K2; LYS-6K2; 

     

     

     


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    In Vitro

    In vitro activity: In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus.

     

    Kinase Assay: LY2584702 Tosylate (also known as LYS6K2) is a novel, selective, orally bioavailable, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. 

     

    Cell Assay: LY-2584702 is fully dissolved in 20 mL 10% DMSO and reserved at -80°C. When conducted the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol and 30% PEG400 to reach different DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. Cell Counting Kit-8 (CCK-8) is used to measure the cells proliferation in vitro. Cell lines A549 and SK-MES-1 treated by LY-2584702 for 24 h with different concentrations are seeded in 96-well plates at a density of 5×103 per well, with six repeats. DMSO treated, or in other words, the concentration of LY-2584702 of 0 is used as negative control. Cells absorbance at 450 nm is detected every 24 h after seeding to measure the proliferative activities[

    In Vivo

    LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.

    Animal model

    Mice

    Formulation & Dosage

    Dissolved in 0.25% Tween-80 and 0.05% antifoam;12.5 mg/kg twice daily, oral

    References

    Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.


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

    LY2584702

    Protein expression of RPS6KB1, p-RPS6KB1, rpS6 and p-rpS6 after the treatment by various LY2584702 concentrations for 24 h.  2017 Aug 9;12(8):e0182891.

    LY2584702

    Proliferation alteration of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702 (CCK-8 analysis).  2017 Aug 9;12(8):e0182891.

    LY2584702

    Cell cycle distribution of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702.  2017 Aug 9;12(8):e0182891.


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