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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.
| Molecular Weight | 564.63 |
| Formula | C29H36N6O6 |
| CAS Number | 496775-62-3 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Cheng G. Expert Rev Hematol. Eltrombopag for the treatment of immune thrombocytopenia.
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Eltrombopag is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR). |
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