Eltrombopag

製品コードS4502 バッチS450204

印刷

化学情報

Chemical Structure Synonyms SB-497115 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H22N4O4
分子量 442.47 CAS No. 496775-61-2
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 7 mg/mL (15.82 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.350mg/ml (0.79mM) Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.050mg/ml (0.11mM) Taking the 1 mL working solution as an example, add 50 μL of 1 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Eltrombopag (SB-497115), a member of the biarylhydrazone class, is a nonpeptide agonist of the thrombopoietin receptor (TpoR), used to treat chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP).
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). This compound activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. It (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. This chemical stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. It also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. This compound increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] It inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] This chemical (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. It (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. This compound (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. It 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] This compound (1 mg/mL) prolongs survival in mouse models of leukemia. [3]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/19038790/
  • https://pubmed.ncbi.nlm.nih.gov/20202683/
  • https://pubmed.ncbi.nlm.nih.gov/22627766/

カスタマーフィードバック

Data from [Data independently produced by , , J Cell Mol Med, 2018, 22(11):5367-5377]

Data from [Data independently produced by , , Int J Oncol, 2015, 47(5):1696-702.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Effects of genetic ablation and pharmacological inhibition of HuR on gene expression, iron metabolism, and hormone levels [ BMC Biol, 2025, 23(1):24] PubMed: 39849491
Eltrombopag Preserves the Clonogenic Potential of Hematopoietic Stem Cells During Treatment With Antithymocyte Globulin in Patients With Aplastic Anemia [ Hemasphere, 2023, 7(6):e906] PubMed: 37304936
Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells [ Am J Cancer Res, 2022, 12(6):2697-2710] PubMed: 35812066
Iron Status Influences the Response of Cord Blood Megakaryocyte Progenitors to Eltrombopag in Vitro [ Blood Adv, 2021, bloodadvances.2021004207] PubMed: 34654056
Eltrombopag inhibits Type I interferon-mediated antiviral signaling by decreasing cellular iron [ Biochem Pharmacol, 2021, 186:114436] PubMed: 33539815
The Thrombopoietin Receptor Agonist Eltrombopag Inhibits Human Cytomegalovirus Replication Via Iron Chelation. [ Cells, 2019, 9(1)] PubMed: 31861948
The synergistic antileukemic effects of eltrombopag and decitabine in myeloid leukemia cells. [ Cancer Manag Res, 2019, 11:8229-8238] PubMed: 31564981
Repurposing the thrombopoietin receptor agonist eltrombopag as an anticryptococcal agent. [ Med Mycol, 2019, myz077] PubMed: 31297540
Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist [Xie C J Cell Mol Med, 2018, 22(11):5367-5377] PubMed: 30156363
Solitary Inhibition of the Breast Cancer Resistance Protein Efflux Transporter Results in a Clinically Significant Drug-Drug Interaction with Rosuvastatin by Causing up to a 2-Fold Increase in Statin Exposure [Elsby R Drug Metab Dispos, 2016, 44(3):398-408] PubMed: 26700956

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。