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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

Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	Click to Expand

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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Handling Instructions

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