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) . Targets thrombopoietin receptor 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. 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.
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Eltrombopag (SB497115) Olamine
Dangerous GoodsCAS number：496775-62-3 molecular formula：C29H36N6O6
overview
compound introduction
Specs
| Chinese alias | 伊屈泼帕乙醇胺盐 | ||
| English alias | 2-Aminoethanol (E)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylate | Promacta (TN) | (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)-2 | ||
| CAS number | 496775-62-3 | molecular formula | C29H36N6O6 |
| molecular weight | 564.63 g/mol | Exact mass | ≥99% |
| PSA | 207.000 Ų | logp | - |
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Safety information
pictogram：
GHS08 , GHS09 , GHS05 , GHS07
Signal word：
Danger
Hazard Statement：
H319: 引起严重眼睛刺激 H373: 通过长时间或反复暴露对器官造成损害 H411: 对水生生物有毒并具有长期持续影响 H412: 对水生生物有害并具有长期持续影响 H302: 吞食有害 H318: 造成严重的眼睛损伤 H400: 对水生生物有剧毒
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P330: 漱口 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P317
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