Eltrombopag
别名: SB-497115 中文名称：艾曲波帕
Eltrombopag (SB-497115),属于biarylhydrazone小分子，是一种thrombopoietin receptor (TpoR)的非肽类激动剂，用于治疗慢性丙型肝炎相关的血小板减少和慢性免疫性(自发的)血小板减少(ITP)。
Eltrombopag Chemical Structure
CAS: 496775-61-2
产品质控
批次：
纯度：
99.99%
99.99
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HEK293/PDZK1 | Function assay | 30 mins | Drug uptake in human OATP1B1 expressing HEK293/PDZK1 cells at 37 degC for 30 mins | 21422191 | |
| HEK293/PDZK1 | Function assay | 30 mins | Drug uptake in human OATP2B1 expressing HEK293/PDZK1 cells at 37 degC for 30 mins | 21422191 | |
| HEK293/PDZK1 | Function assay | 30 mins | Drug uptake in human OCT1 expressing HEK293/PDZK1 cells at 37 degC for 30 mins | 21422191 | |
| VERO-E6 | Function assay | 48 hrs | Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=3.26μM | ChEMBL | |
| Vero | Antiviral assay | 24 hrs | Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=8.27μM | ChEMBL | |
| Ba/F3 | Function assay | Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assay, EC50=0.038μM | 18783949 | ||
| Ba/F3 | Function assay | Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expression, EC50=0.038μM | 18778936 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP2B1-mediated [3H]estrone-3-sulfate uptake in human OATP2B1 expressing HEK293/PDZK1 cells by scintillation counting, Ki=8.48μM | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP1B1-mediated [3H]estrone-3-sulfate uptake in human OATP1B1 expressing HEK293/PDZK1 cells by scintillation counting, Ki=14.9μM | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP1B3-mediated [3H]estradiol 17beta-glucuronide uptake in human OATP1B3 expressing HEK293/PDZK1 cells by scintillation counting, Ki=25.6μM | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP1B3-mediated [3H]estradiol 17beta-glucuronide uptake in human OATP1B3 expressing HEK293/PDZK1 cells by scintillation counting | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OCT1-mediated [14C]tetraethylammonium uptake in human OCT1 expressing HEK293/PDZK1 cells by scintillation counting | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP1B1-mediated [3H]estrone-3-sulfate uptake in human OATP1B1 expressing HEK293/PDZK1 cells by scintillation counting | 21422191 | ||
| HEK293/PDZK1 | Function assay | Inhibition of OATP2B1-mediated [3H]estrone-3-sulfate uptake in human OATP2B1 expressing HEK293/PDZK1 cells by scintillation counting | 21422191 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Eltrombopag (SB-497115),属于biarylhydrazone小分子，是一种thrombopoietin receptor (TpoR)的非肽类激动剂，用于治疗慢性丙型肝炎相关的血小板减少和慢性免疫性(自发的)血小板减少(ITP)。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 含有STAT激活的IRF-1启动子和人TpoR (BAF3/IRF-1/hTpoR)调控的转染荧光素酶报告基因的小鼠BAF3细胞中，Eltrombopag表现出的半数最大有效浓度(EC50) 为0.27 μM。Eltrombopag通过结合金属铁(i.e., Zn2+)和TpoR的跨膜与近膜结构域内特异性氨基酸，从而激活受体。抗磷酸- STAT5抗体免疫印迹检测表明，Eltrombopag (30 μM)激活N2C-Tpo 细胞中STAT5。培育2天后，Eltrombopag刺激增殖，对BAF3/hTpoR细胞进行BrdU测定，EC50为0.03 μM。Eltrombopag也会诱导造血干细胞分化为巨核祖细胞。Eltrombopag剂量依赖性增加骨髓CD34+细胞分化为CD41+巨核细胞，EC50为0.1 μM。[1] Eltrombopag抑制N2C-Tpo细胞和HEL92.1.7细胞增殖，IC50分别为20.7 μg/mL和2.3 μg/mL。[2]在人和小鼠白血病细胞中，Eltrombopag (20 μg/mL)导致细胞分裂率减少，细胞周期G(1)期阻滞，以及细胞分化增加。HL60 细胞中，Eltrombopag (5 μg/mL)表现出明显的分化信号，显著改变细胞核内容物的结构，并增加细胞质/细胞核比率。Eltrombopag (5 μg/mL)增加CD11b，这与U937细胞中前巨噬细胞状态一致，并引起URE细胞中CD11b的增加。白血病HL60细胞中，Eltrombopag导致细胞内游离铁离子剂量依赖性减少。[3] | |||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK p-RB / RB / CDK4 / CDK6 / Cyclin D1 |
|
30156363 | |
| Growth inhibition assay | Cell viability |
|
31564981 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Eltrombopag (10 mg/kg每天) 最后一次给药1周后，使一只黑猩猩体内的血细胞数量大约增加超过2倍，另外两只黑猩猩体内大约增加1.5倍。[1] Eltrombopag (1 mg/mL)延长白血病小鼠模型的存活时间。[3] | |
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05961410 | Recruiting | Lymphoma|Peripheral Blood Stem Cell Transplantation |
National Taiwan University Hospital|Novartis |
August 15 2023 | Phase 2 |
| NCT05653219 | Recruiting | Primary Immune Thrombocytopenia |
Novartis Pharmaceuticals|Novartis |
January 21 2023 | Phase 3 |
| NCT05049668 | Enrolling by invitation | Severe Aplastic Anemia |
European Society for Blood and Marrow Transplantation |
October 2021 | -- |
化学信息&溶解度
| 分子量 | 442.47 | 分子式 | C25H22N4O4 |
| CAS号 | 496775-61-2 | SDF | Download Eltrombopag SDF |
| Smiles | CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N=NC3=CC=CC(=C3O)C4=CC(=CC=C4)C(=O)O)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 11 mg/mL ( (24.86 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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