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About This Item
Empirical Formula (Hill Notation):
C25H22N4O4·2C2H7NO
CAS Number:
Molecular Weight:
564.63
MDL number:
NACRES:
NA.21
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
light brown-red to very dark brown-red
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active, potent and selective thrombopoietin (Tpo) receptor (TpoR) agonist in vitro and in vivo.
Eltrombopag is an orally active nonpeptide thrombopoietin receptor (TpoR) agonist that selectively induces STAT activation and proliferation (EC50 = 270 & 30 nM, respectively) of hToR-transfected, but not non-transfected, BAF3 cells. Eltrombopag increases the differentiation of primary human CD34(+) bone marrow cells into CD41(+) megakaryocytes ex vivo (EC50 = 100 nM) and exhibits thrombopoietic activity in chimpanzees in vivo (10 mg/kg/day p.o.).
Eltrombopag is an orally active nonpeptide thrombopoietin receptor (TpoR) agonist that selectively induces STAT activation and proliferation (EC50 = 270 & 30 nM, respectively) of hToR-transfected, but not non-transfected, BAF3 cells. Eltrombopag increases the differentiation of primary human CD34(+) bone marrow cells into CD41(+) megakaryocytes ex vivo (EC50 = 100 nM) and exhibits thrombopoietic activity in chimpanzees in vivo (10 mg/kg/day p.o.).
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Connie L Erickson-Miller et al.
Stem cells (Dayton, Ohio), 27(2), 424-430 (2008-11-29)
Eltrombopag is a first-in-class, orally bioavailable, small-molecule, nonpeptide agonist of the thrombopoietin receptor (TpoR), which is being developed as a treatment for thrombocytopenia of various etiologies. In vitro studies have demonstrated that the activity of eltrombopag is dependent on expression
Gabriel Levy et al.
Blood, 135(12), 948-953 (2020-01-25)
Mutations in the MPL gene encoding the human thrombopoietin receptor (TpoR) drive sporadic and familial essential thrombocythemias (ETs). We identified 2 ET patients harboring double mutations in cis in MPL, namely, L498W-H499C and H499Y-S505N. Using biochemical and signaling assays along
Eltrombopag inhibits the proliferation of Ewing sarcoma cells via iron chelation and impaired DNA replication
Waters T, et al.
BMC Cancer, 20 (2020)
Darren Kelly et al.
Journal of veterinary internal medicine, 34(2), 890-892 (2020-02-26)
Idiopathic aplastic pancytopenia is an uncommon disease in dogs which results in pancytopenia and for which an immune-mediated etiology is suspected. A small number of affected dogs reported in the veterinary literature have responded to immunosuppressive medication but the prognosis
Gavin C Sampey et al.
Viruses, 12(10) (2020-09-27)
Human immunodeficiency virus 1 (HIV-1) is the most prevalent human retrovirus. Recent data show that 34 million people are living with HIV-1 worldwide. HIV-1 infections can lead to AIDS which still causes nearly 20,000 deaths annually in the USA alone.
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