Eltrombopag

Catalog No.S4502 Batch:S450204

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Technical Data

Formula

C25H22N4O4
Molecular Weight 442.47 CAS No. 496775-61-2
Solubility (25°C)* In vitro DMSO 7 mg/mL (15.82 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Eltrombopag (SB-497115), a member of the biarylhydrazone class, is a nonpeptide agonist of the thrombopoietin receptor (TpoR), used to treat chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP).
Targets
thrombopoietin receptor (TpoR) [1]
In vitro Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. [3]
In vivo Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. [1] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [3]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , J Cell Mol Med, 2018, 22(11):5367-5377]

Data from [Data independently produced by , , Int J Oncol, 2015, 47(5):1696-702.]

Selleck's Eltrombopag has been cited by 10 publications

Eltrombopag Preserves the Clonogenic Potential of Hematopoietic Stem Cells During Treatment With Antithymocyte Globulin in Patients With Aplastic Anemia [ Hemasphere, 2023, 7(6):e906] PubMed: 37304936
Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells [ Am J Cancer Res, 2022, 12(6):2697-2710] PubMed: 35812066
Iron Status Influences the Response of Cord Blood Megakaryocyte Progenitors to Eltrombopag in Vitro [ Blood Adv, 2021, bloodadvances.2021004207] PubMed: 34654056
Eltrombopag inhibits Type I interferon-mediated antiviral signaling by decreasing cellular iron [ Biochem Pharmacol, 2021, 186:114436] PubMed: 33539815
The Thrombopoietin Receptor Agonist Eltrombopag Inhibits Human Cytomegalovirus Replication Via Iron Chelation. [ Cells, 2019, 9(1)] PubMed: 31861948
The synergistic antileukemic effects of eltrombopag and decitabine in myeloid leukemia cells. [ Cancer Manag Res, 2019, 11:8229-8238] PubMed: 31564981
Repurposing the thrombopoietin receptor agonist eltrombopag as an anticryptococcal agent. [ Med Mycol, 2019, myz077] PubMed: 31297540
Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist [Xie C J Cell Mol Med, 2018, 22(11):5367-5377] PubMed: 30156363
Solitary Inhibition of the Breast Cancer Resistance Protein Efflux Transporter Results in a Clinically Significant Drug-Drug Interaction with Rosuvastatin by Causing up to a 2-Fold Increase in Statin Exposure [Elsby R Drug Metab Dispos, 2016, 44(3):398-408] PubMed: 26700956
Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure [Elsby R, et al. Drug Metab Dispos, 2015, 44(3):398-408] PubMed: 26700956

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.