Substance
ID:73323
Names and Identifiers
Synonyms
RevoladePromactaSB-497115-GREltrombopag
IUPAC Traditional name
eltrombopag
IUPAC name
3-(3-{2-[(4E)-1-(3,4-dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-ylidene]hydrazin-1-yl}-2-hydroxyphenyl)benzoic acid
Registration numbers
CAS Number
Properties
Product Information
Salt Data
Free Base
Safety Information
Storage Condition
-20°C
Pharmacology Properties
Target
TpoR
Molecule Details
Research Area: Cancer
Biological Activity:
Eltrombopag (SB-497115-GR, Promacta, Revolade) is a small molecule agonist of the c-mpl (TpoR) receptor with an IC50 of 0.69 μM for the inhibition of hERG K+ channel tail current. In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts.In addition, eltrombopag (SB-497115-GR, Promacta, Revolade) decreased proliferation of all cancer cell lines. [1][2]
Biological Activity:
Eltrombopag (SB-497115-GR, Promacta, Revolade) is a small molecule agonist of the c-mpl (TpoR) receptor with an IC50 of 0.69 μM for the inhibition of hERG K+ channel tail current. In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts.In addition, eltrombopag (SB-497115-GR, Promacta, Revolade) decreased proliferation of all cancer cell lines. [1][2]
Molecular Spectra
No Data Available
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References
• Erickson-Miller CL et al. Leuk Res. 2010 Sep;34(9):1224-31.