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Eltrombopag

別名: SB-497115 中文名稱：艾曲波帕

Eltrombopag (SB-497115),屬于biarylhydrazone小分子，是一種thrombopoietin receptor (TpoR)的非肽類激動(dòng)劑，用于治療慢性丙型肝炎相關(guān)的血小板減少和慢性免疫性(自發(fā)的)血小板減少(ITP)。

Eltrombopag Chemical Structure

Eltrombopag Chemical Structure

CAS: 496775-61-2

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 810.81 現(xiàn)貨
10mg 806.02 現(xiàn)貨
50mg 2445.87 現(xiàn)貨
200mg 5716.72 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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Eltrombopag 相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Eltrombopag (SB-497115),屬于biarylhydrazone小分子，是一種thrombopoietin receptor (TpoR)的非肽類激動(dòng)劑，用于治療慢性丙型肝炎相關(guān)的血小板減少和慢性免疫性(自發(fā)的)血小板減少(ITP)。
靶點(diǎn)
thrombopoietin receptor (TpoR) [1]
體外研究(In Vitro)
體外研究活性 含有STAT激活的IRF-1啟動(dòng)子和人TpoR (BAF3/IRF-1/hTpoR)調(diào)控的轉(zhuǎn)染熒光素酶報(bào)告基因的小鼠BAF3細(xì)胞中，Eltrombopag表現(xiàn)出的半數(shù)最大有效濃度(EC50) 為0.27 μM。Eltrombopag通過(guò)結(jié)合金屬鐵(i.e., Zn2+)和TpoR的跨膜與近膜結(jié)構(gòu)域內(nèi)特異性氨基酸，從而激活受體?？沽姿? STAT5抗體免疫印跡檢測(cè)表明，Eltrombopag (30 μM)激活N2C-Tpo 細(xì)胞中STAT5。培育2天后，Eltrombopag刺激增殖，對(duì)BAF3/hTpoR細(xì)胞進(jìn)行BrdU測(cè)定，EC50為0.03 μM。Eltrombopag也會(huì)誘導(dǎo)造血干細(xì)胞分化為巨核祖細(xì)胞。Eltrombopag劑量依賴性增加骨髓CD34+細(xì)胞分化為CD41+巨核細(xì)胞，EC50為0.1 μM。[1] Eltrombopag抑制N2C-Tpo細(xì)胞和HEL92.1.7細(xì)胞增殖，IC50分別為20.7 μg/mL和2.3 μg/mL。[2]在人和小鼠白血病細(xì)胞中，Eltrombopag (20 μg/mL)導(dǎo)致細(xì)胞分裂率減少，細(xì)胞周期G(1)期阻滯，以及細(xì)胞分化增加。HL60 細(xì)胞中，Eltrombopag (5 μg/mL)表現(xiàn)出明顯的分化信號(hào)，顯著改變細(xì)胞核內(nèi)容物的結(jié)構(gòu)，并增加細(xì)胞質(zhì)/細(xì)胞核比率。Eltrombopag (5 μg/mL)增加CD11b，這與U937細(xì)胞中前巨噬細(xì)胞狀態(tài)一致，并引起URE細(xì)胞中CD11b的增加。白血病HL60細(xì)胞中，Eltrombopag導(dǎo)致細(xì)胞內(nèi)游離鐵離子劑量依賴性減少。[3]
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Eltrombopag (10 mg/kg每天) 最后一次給藥1周后，使一只黑猩猩體內(nèi)的血細(xì)胞數(shù)量大約增加超過(guò)2倍，另外兩只黑猩猩體內(nèi)大約增加1.5倍。[1] Eltrombopag (1 mg/mL)延長(zhǎng)白血病小鼠模型的存活時(shí)間。[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 --

化學(xué)信息&溶解度

分子量 442.47 分子式

C25H22N4O4
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 11 mg/mL ( (24.86 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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