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    LY2409881 trihydrochloride
    LY2409881 trihydrochloride

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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 #: V0757
    CAS #: 946518-60-1 Purity ≥98%

    Description: LY2409881  trihydrochloride (LY-2409881; LY 2409881), the trihydrochloride salt of LY-2409881, is a novel, potent and selective IKK2 ( IκB kinase β) inhibitor with potential anticancer and anti-inflammatory activity. It inhibits IKK2 ( IκB kinase β) with an IC50 of 30 nM, and exhibits >10-fold selectivity for inhibiting IKK2 over IKK1 and other closely related kinases. LY2409881 significantly inhibited tumor growth in vivo in SCID-beige xenograft mouse model. LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. LY2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. LY2409881 suppressed the activity of the NF-κB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs.

    References: Clin Cancer Res. 2015 Jan 1;21(1):134-45.

    Related CAS: 946518-61-2 (free base)

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    Molecular Weight (MW)594.43
    FormulaC24H32Cl4N6OS
    CAS No.946518-60-1 (3HCl); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (33.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    SynonymsLY2409881 tri-HCl; LY-2409881; LY 2409881; LY2409881 trihydrochloride

    Chemical Name: 2-(5-chloro-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride

    InChi Key: IEXCRLAGBWKVPW-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H29ClN6OS.3ClH/c1-30-10-12-31(13-11-30)9-3-8-26-24-27-15-19(25)22(29-24)21-14-18-17(4-2-5-20(18)33-21)23(32)28-16-6-7-16;;;/h2,4-5,14-16H,3,6-13H2,1H3,(H,28,32)(H,26,27,29);3*1H

    SMILES Code: O=C(C1=C(C=C(C2=NC(NCCCN3CCN(C)CC3)=NC=C2Cl)S4)C4=CC=C1)NC5CC5.[H]Cl.[H]Cl.[H]Cl           


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    In Vitro

    In vitro activity: LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth.


    Kinase Assay: LY2409881 is an IKK2 inhibitor that inhibits TNFα-induced activation of NF-κB. By in vitro kinase assay, LY2409881 potently inhibits IKK2, with an IC50 of 30 nM. In contrast, the IC50 for IKK1 and other common kinases is at least one log higher. The specificity of LY2409881 for NF-κB signaling is further studied in a cell-based assay, by examining the effect of LY2409881 in the TNFα-dependent antiapoptosis function. TNFα is a well-characterized upstream stimulus of NF-κB.


    Cell Assay: Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.

    In VivoIn SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, i.p.) significantly inhibits the tumor growth 
    Animal modelIn SCID-beige mice bearing LY10 cell-derived tumors
    Formulation & Dosage50, 100 and 200 mg/kg
    ReferencesClin Cancer Res. 2015 Jan 1;21(1):134-45


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

     

    LY2409881

    Novel IKK2 inhibitor, LY2409881, blocked the activation of NF-κB in response to TNFα. Clin Cancer Res. 2015 Jan 1;21(1):134-45. 
     

    LY2409881

    LY2409881 inhibited constitutively activated NF-κB and caused apoptosis in models of B- and T-cell lymphoma. Clin Cancer Res. 2015 Jan 1;21(1):134-45. 
     

    LY2409881

    LY2409881 inhibited DLBCL cells in vitro and in vivo. Clin Cancer Res. 2015 Jan 1;21(1):134-45. 
     

    LY2409881

    LY2409881 was synergistic with doxorubicin, cyclophosphamide, and HDAC inhibitors. Clin Cancer Res. 2015 Jan 1;21(1):134-45. 
     

    LY2409881

    The distinct effects of LY2409881 and HDAC inhibitors on p65/RelA, and the expression of HDACs in DLBCL. Clin Cancer Res. 2015 Jan 1;21(1):134-45. 


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