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    Eltrombopag (SB-497115)
    Eltrombopag (SB-497115)

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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 #: V1896
    CAS #: 496775-61-2 Purity ≥98%

    Description: Eltrombopag (formerly SB-497115; SB 497115; SB497115; trade name PROMACTA), a member of the biarylhydrazone class, is a novel nonpeptide agonist of the thrombopoietin receptor (TpoR) approved for use in the treatment of chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP). Eltrombopag demonstrates an EC50 of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR. Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR.

    References: Stem Cells. 2009 Feb;27(2):424-30; Leuk Res. 2010 Sep;34(9):1224-31; Blood. 2012 Jul 12;120(2):386-94. 

    Related CAS#: 496775-62-3 (olamine); 496775-61-2 (free base)

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    Molecular Weight (MW)442.47 
    FormulaC25H22N4O4 
    CAS No.496775-61-2 (free base); 496775-61-2 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 26 mg/mL (58.8 mM)           
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Exact Mass: 442.16411 

    Chemical Name: 3'-[2-[(2Z)-1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid

    SMILES Code: O=C(C1=CC(C2=CC=CC(N/N=C3C(C)=NN(C4=CC=C(C)C(C)=C4)C/3=O)=C2O)=CC=C1)O
    SynonymsEltrombopag; SB497115; SB-497115; SB 497115; SB497115GR; trade name: PROMACTA


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    In Vitro

    In vitro activity: Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL. Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells.


    Cell Assay:  Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells.

    In VivoEltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. 
    Animal modelMouse models of leukemia. 
    Formulation & Dosage10 mg/kg
    ReferencesStem Cells. 2009 Feb;27(2):424-30; Leuk Res. 2010 Sep;34(9):1224-31; Blood. 2012 Jul 12;120(2):386-94.  


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

    Eltrombopag

    Signal transduction induced by eltrombopag. Stem Cells. 2009 Feb;27(2):424-30.
     

    Eltrombopag

    Proliferation and differentiation induced by eltrombopag. Stem Cells. 2009 Feb;27(2):424-30.
     

    Eltrombopag

    Additive effects of eltrombopag and rhTpo. Stem Cells. 2009 Feb;27(2):424-30.


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