Eltrombopag

Synonyms: SB-497115

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).

Eltrombopag  Chemical Structure

Eltrombopag Chemical Structure

CAS: 496775-61-2

Selleck's Eltrombopag has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Eltrombopag Related Products

Choose Selective TpoR Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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).
Targets
thrombopoietin receptor (TpoR) [1]
In vitro
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. [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]
Experimental Result Images Methods Biomarkers Images 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
In Vivo
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] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [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
February 2 2023 Phase 3
NCT05049668 Enrolling by invitation
Severe Aplastic Anemia
European Society for Blood and Marrow Transplantation
October 2021 --

Chemical Information & Solubility

Molecular Weight 442.47 Formula

C25H22N4O4

CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 11 mg/mL ( (24.86 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Eltrombopag | Eltrombopag ic50 | Eltrombopag price | Eltrombopag cost | Eltrombopag solubility dmso | Eltrombopag purchase | Eltrombopag manufacturer | Eltrombopag research buy | Eltrombopag order | Eltrombopag mouse | Eltrombopag chemical structure | Eltrombopag mw | Eltrombopag molecular weight | Eltrombopag datasheet | Eltrombopag supplier | Eltrombopag in vitro | Eltrombopag cell line | Eltrombopag concentration | Eltrombopag nmr