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Eltrombopag

Name: Eltrombopag
Brand: Selleck Chemicals
SKU: S4502
Rating: 5 (9 reviews)

Synonyms: SB-497115

Catalog No.S4502 Purity:99.99%

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

CAS No. 496775-61-2

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Eltrombopag Related Products

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Cell Data

Cell Lines	Assay Type	Incubation Time	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

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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

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