| Name | Eltrombopag |
| Description | Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110). |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.26 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 10 mg/mL (22.6 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| Keywords | Thrombopoietin receptor | SB497115 | SB 497115 | N2C-Tpo | megakaryocyte | Inhibitor | inhibit | immune thrombocytopenia | hepatocellular carcinomab | hematopoiesis | Eltrombopag | chimpanzee | CD34 | blood platelet | BAF3 | Bacterial | Apoptosis |
| Inhibitors Related | Neomycin sulfate | Aceglutamide | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Imidazole | Formamide | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
