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Cat. No. Name Size Price Add Cart
KI1117Eltrombopag5 mg$192
Eltrombopag10 mg$336
Eltrombopag50 mg$1072
Eltrombopag200 mg$2992

Chemical Characteristic

Product NameEltrombopag
SynonymsSB-497115-GR, SB-497115, Revolade
CAS No.496775-61-2
Molecular Weight 442.47
FormulaC25H22N4O4
Chemical Name3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid
Smilesc1(cc(ccc1)C(=O)O)c1c(c(ccc1)N/N=C\1/C(=NN(C1=O)c1cc(c(cc1)C)C)C)O
Chemical Structure

Biological activities

Eltrombopag is a small molecule nonpeptide agonist of the thrombopoietin receptor (TpoR). The EC50 of eltrombopag is 0.27 µM in murine BAF3 cells transfected with tluciferase reporter gene. Eltrombopag exhibits no activity in cells expressing receptors for hematopoietic growth factors that are activated by STAT, including Epo, G-CSF, interferon (IFN)-, and IL-3. Eltrombopag at a 30-µM concentration activates STAT5 in N2C-Tpo cells. Eltrombopag at the dose of 10 µM also activates p42/44 MAPK with similar kinetics to rhTpo (50 ng/mL). In a BrdU assay conducted in BAF3/hTpoR cells, eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 30 nM. Eltrombopag prevents the apoptosis of Tpo-dependent cells. Eltrombopag is well tolerated following repeat oral doses. [1] Eltrombopag decreases proliferation of non-small cell lung carcinoma (NSCLC) cell lines including A549, EKVX, HOP-62 after 72-hour culture with an IC50 ranging from 5.7 to 14 µg/mL.[2] Eltrombopag increases platelet production through activation of the thrombopoietin receptor.[3] Eltrombopag induces the phosphorylation signal transducers and activators of transcription (STAT) proteins with no phosphorylation of Akt.[4]

Protocols

In vitro Eltrombopag (SB-497115) is dissolved in dimethyl sulfoxide.[4]

References

[1] Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009, 27(2): 424-430.
[2] Erickson-Miller CL, et al. Effect of eltrombopag on proliferation of solid and hematologic tumor cell lines in vitro. Journal of Clinical Oncology, 2008, 26, 15S: 14628.
[3] Nieto M, et al. The European Medicines Agency review of eltrombopag (Revolade) for the treatment of adult chronic immune (idiopathic) thrombocytopenic purpura: summary of the scientific assessment of the Committee for Medicinal Products for Human Use. Haematologica. 2011 Sep;96(9): e33-e40.
[4] Erhardt JA, et al. Comparative analyses of the small molecule thrombopoietin receptor agonist eltrombopag and thrombopoietin on in vitro platelet function. Exp Hematol. 2009, 37(9): 1030-1037.

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