A thrombopoietin receptor agonist and iron chelator
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Eltrombopag

Item No. 13247

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
496775-61-2
Synonyms
  • SB 497115
Molecular Formula
C25H22N4O4
Formula Weight
442.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 20 mg/mlEthanol: 0.1 mg/mlPBS (pH 7.2): Slightly soluble
λmax
248, 417 nm
SMILES
OC1=C(N/N=C2C(N(C3=CC(C)=C(C)C=C3)N=C\2C)=O)C=CC=C1C4=CC(C(O)=O)=CC=C4
InChi Code
InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22-
InChi Key
XDXWLKQMMKQXPV-QYQHSDTDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.1 It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.2 It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Erickson-Miller, C.L., Delorme, E., Tian, S.S., et al. Preclinical activity of eltrombopag (SB-497115), an oral, non-peptide thrombopoietin receptor agonist. Stem Cells 27(2), 424-430 (2008).

    2. Vlachodimitropoulou, E., Chen, Y.L., Garbowski, M., et al. Eltrombopag: A powerful chelator of cellular or extracellular iron(III) alone or combined with a second chelator. Blood 130(17), 1923-1933 (2017).