Eltrombopag

SKU: orb1305316

Description

Eltrombopag

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 496775-61-2
• MW: 442.47
• Purity: 98.00%
• Formula: C₂₅H₂₂N₄O₄
• SMILES: O=C/1N(N=C(C)\C1=N\NC2=C(O)C(=CC=C2)C3=CC(C(O)=O)=CC=C3)C4=CC(C)=C(C)C=C4
• Target: Thrombin,Apoptosis,Antibacterial,Thrombopoietin Receptor
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:10 mg/mL (22.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.26 mM)

Bioactivity

• 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. Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia.
• 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. Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Thrombopoietin receptor, Thrombopoietin Receptor, SB497115, SB-497115, SB-497115-GR, SB 497115, megakaryocyte, hepatocellular carcinomab, hematopoiesis, Eltrombopag, N2C-Tpo, immune thrombocytopenia, inhibit, Inhibitor, chimpanzee, CD34, Apoptosis, BAF3, Bacterial, blood platelet

Compound Identifiers

PubChem CID

135449332