中文名：艾曲波帕乙醇胺
英文名：Eltrombopag (SB497115) Olamine
英文別名：SB-497115-GR;3'-[(2Z)-2-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-Biphenyl]-3-carboxylic acid compd.with 2-aminoethanol (1:2)
純度：10mM in DMSO
貨號(hào)：E407823
包裝：1ml
Cas號(hào)：496775-62-3
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
Information
Eltrombopag (SB497115) Olamine Eltrombopag Olamine (SB-497115-GR, SB497115) is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR) .
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. Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia.
Cell?Data
cell?lines：HeLa cells
Concentrations：
Incubation?Time：
Powder?Purity:≥99%
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關(guān)鍵字： SB-497115-GR;3'-[(2Z)-2-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-Biphenyl]-3-carboxylic acid compd.with 2-aminoethanol (1:2)
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