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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Eltrombopag
Eltrombopag
  • Eltrombopag

Eltrombopag NEW

Price $48 $67 $119
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-14

Product Details

Product Name: Eltrombopag CAS No.: 496775-61-2
Purity: 99.73% Supply Ability: 10g
Release date: 2024/11/14

Product Introduction

Bioactivity

名稱Eltrombopag
描述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).
體外活性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]
體內(nèi)活性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]
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 4.42 mg/mL (10 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字hepatocellular carcinomab | Apoptosis | Inhibitor | hematopoiesis | chimpanzee | inhibit | SB497115 | immune thrombocytopenia | CD34 | blood platelet | BAF3 | Thrombopoietin Receptor | Bacterial | N2C-Tpo | megakaryocyte | SB 497115 | Eltrombopag
相關(guān)產(chǎn)品(S)-(+)-Ibuprofen | AEBSF hydrochloride | Heparin sodium salt
相關(guān)庫經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | FDA 上市藥物庫 | 抗癌活性化合物庫 | 抗癌藥物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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