Cat. No.: HY-15306

Eltrombopag

(Synonyms: SB-497115)

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.

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Pureté: 99.94%
CAS No.: 496775-61-2
Formule: C₂₅H₂₂N₄O₄
Masse moléculaire:442.47

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Eltrombopag Chemical Structure

CAS No.: 496775-61-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Thrombopoietin Receptor, Staphylococcus aureus, Apoptosis^[1]^[3]^[5]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	0.038 μM Compound: 1	Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expression Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expression	[PMID: 18778936]
BaF3	EC₅₀	0.038 μM Compound: 1	Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assay Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assay	[PMID: 18783949]
MOLM-13	GI₅₀	8.28 μM Compound: 11a	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition	[PMID: 36692498]
Vero	CC₅₀	>50 μM Compound: Eltombopag	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	8.27 μM Compound: Eltombopag	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene^[1].
Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells^[1].
Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes^[1].
Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells^[1].
Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34⁺ cells into CD41⁺ megakaryocytes^[1].
Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis^[1].
Eltrombopag efficiently inhibits Pneumococcal growth with MIC₅₀ of 0.3 mg/L, but shows no activity against Gram-negative bacteria^[3].
Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibits Staphylococcus aureus growth with an MIC₅₀ of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC₅₀ of 1.2 mg/L^[3].
Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells^[5].
Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

Murine BAF3 cells
Concentration:

0.002-50 μM
Incubation Time:

4 h
Result:

Effectively inhibited murine BAF3 cells with human TpoR with an EC₅₀ value of 0.27 μM.

^[1]^[1]

Cell Line:

N2C-Tpo cells and CD34⁺
Concentration:

30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34⁺
Incubation Time:

120 min for N2C-Tpo cells; 30 min for CD34⁺
Result:

Activated phospho-STAT5 and maximum signal intensity exhibited at 60 minutes after treatment in N2C-Tpo cells.
Dose-dependently activated STAT5 phosphorylation at 30 minutes after treatment in CD34⁺.

Cell Proliferation Assay^[1]

Cell Line:

BAF3/hTpoR cells
Concentration:

0.1 nM-10 μM
Incubation Time:

2 days
Result:

Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM.

Cell Differentiation Assay^[1]

Cell Line:

CD34⁺
Concentration:

0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time:

10 days
Result:

Dose-dependently stimulated the differentiation from bone marrow CD34⁺ cells to CD41⁺ megakaryocytes with an EC50 value of 0.1 μM.

Apoptosis Analysis^[1]

Cell Line:

N2C-Tpo cells
Concentration:

0, 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time:

72 hours
Result:

Exhibited dose-dependently antiapoptotic effects N2C-Tpo cells with a concentration over 0.03 μM.

Cell Proliferation Assay^[5]

Cell Line:

Huh7, HepG2 and Hep3B cells (preloaded with iron (500 μg/ml FAC) for 24 h)
Concentration:

0.1-100 μg/mL
Incubation Time:

72 h
Result:

Exhibited anti-proliferative activity against HCC cell lines with IC₅₀s of 5.7 μg/ml for Huh7, 5.4 μg/ml for HepG2, and 4.7 μg/ml for Hep3B.

Cell Cycle Analysis^[5]

Cell Line:

Huh7 cells
Concentration:

0 or 10 μg/mL
Incubation Time:

72 h
Result:

Significantly induced G0/G1 phase arrest.

In Vivo

Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees^[1].
Eltrombopag Olamine (17.6 mg/kg; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female chimpanzees^[1]
Dosage:

10 mg/kg
Administration:

Oral gavage; 10 mg/kg once a day; for 5 days
Result:

Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.

Animal Model:

C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 10⁸ CFU suspended in 40 µL PBS) into the nasal cavities)^[3]
Dosage:

17.6 mg/kg
Administration:

IP; once a day for 2 days
Result:

Significantly reduced mean bacterial counts (5.0 × 10⁶ CFU/lung) in the nasal infection model compared with control PBS (5.2 × 10⁷ CFU/lung) mice.

Chemical Information

CAS No. 496775-61-2
Appearance Solid
Masse moléculaire 442.47
Formule C₂₅H₂₂N₄O₄
Color Yellow to orange
SMILES

O=C(C1=CC(C2=CC=CC(N/N=C3C(C)=NN(C4=CC=C(C)C(C)=C4)C/3=O)=C2O)=CC=C1)O
Synonyms

SB-497115
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

All IFIn Vivo Efficacy StudyRT-PCRWB

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Journal Impact Factor

Cell

Rational discovery of therapeutic PAK1 allosteric activators. [Abstract]

2026 May 28;189(11):3444-3464.e28. PMID: 41923641
ACS Nano

Long Noncoding RNA NR_030777 Alleviates Cobalt Nanoparticles-Induced Neurodegenerative Damage by Promoting Autophagosome-Lysosome Fusion. [Abstract]

2024 Sep 10;18(36):24872-24897. PMID: 39197041

Eltrombopag purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Sep 10;18(36):24872-24897. [Abstract]

The level of tau phosphorylation after pretreated with 20 μM Eltrombopag.
Neuron

CLN3 mediates chloride efflux from lysosomes. [Abstract]

2026 Mar 4;114(5):868-883.e7. PMID: 41558486
Cell Death Discov

CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]

2024 Oct 26;10(1):453. PMID: 39461947
J Transl Med

Single-cell profiling of SLC family transporters: uncovering the role of SLC7A1 in osteosarcoma. [Abstract]

2025 Jan 22;23(1):103. PMID: 39844299
Int J Surg

Apoptotic extracellular vesicles from peripancreatic adipose-derived mesenchymal stem cells ameliorate severe acute pancreatitis through the transcription factor EB-mediated autophagy-lysosomal pathway: an experimental study. [Abstract]

2025 Dec 17. PMID: 41403290
Alzheimers Res Ther

Intermittent hypoxia training enhances Aβ endocytosis by plaque associated microglia via VPS35-dependent TREM2 recycling in murine Alzheimer's disease. [Abstract]

2024 Jun 3;16(1):121. PMID: 38831312

Eltrombopag purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2024 Jun 3;16(1):121. [Abstract]

Brain sections of APP/PS1 mice treated with IHT or EO (Eltrombopag, i.p., 30 mg/kg/day for 14d) were probed with 6E10 antibodies, and microscopy images of the Aβ plaques were acquired. White arrows indicate plaques. Scale bar =2 mm.

Eltrombopag purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2024 Jun 3;16(1):121. [Abstract]

Brain sections of IHT or EO (Eltrombopag, i.p., 30 mg/kg/day for 14d)-treated APP/PS1 mice were stained with anti-VPS35 and anti-Iba1 antibodies, and microscopy images of DAM in CA1 region were captured. Scale bar =20 μm.

Eltrombopag purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2024 Jun 3;16(1):121. [Abstract]

Number of Aβ plaques in the hippocampus of APP/PS1 mice treated with IHT or EO (Eltrombopag, i.p., 30 mg/kg/day for 14d).
Cell Rep

IRE1α regulates macrophage phagocytosis in immune thrombocytopenia through NR1D1 mRNA decay and lysosomal biogenesis. [Abstract]

2026 Mar 12;45(3):117083. PMID: 41824452
Blood Adv

Novel TPO receptor agonist TA-316 contributes to platelet biogenesis from human iPS cells. [Abstract]

2017 Feb 28;1(7):468-476. PMID: 29296963

Eltrombopag purchased from MedChemExpress. Usage Cited in: Blood Adv. 2017 Feb 28;1(7):468-476. [Abstract]

STAT5 phosphorylation in UT-7/TPO cells stimulated for 15 to 360 minutes with rhTPO (100 ng/mL), TA-316 (100 ng/mL), Eltrombopag (1000 ng/mL), or DMSO (vehicle) are evaluated using BD Phosflow (STAT5, pY694).
Acta Neuropathol Commun

Transaldolase 1 impacts Parkinson's disease pathogenesis via metabolic reprogramming and autophagy-lysosomal pathway. [Abstract]

2025 Nov 4;13(1):223. PMID: 41189023
Cells

Assessment of FDA-Approved Drugs as a Therapeutic Approach for Niemann-Pick Disease Type C1 Using Patient-Specific iPSC-Based Model Systems. [Abstract]

2022 Jan 18;11(3):319. PMID: 35159129
Eur J Pharmacol

Eltrombopag restores proliferative capacity and adipose-osteogenic balance of mesenchymal stromal cells in low-risk myelodysplastic syndromes. [Abstract]

2024 Oct 29:177086. PMID: 39481629
Front Pharmacol

Correlation of the Plasma Concentration of Eltrombopag With Efficacy in the Treatment of Refractory Aplastic Anemia: A Single-Centre Study in China. [Abstract]

2020 Nov 16:11:582625. PMID: 33364958
J Thromb Haemost

Generation of a thrombopoietin-deficient thrombocytopenia model in zebrafish. [Abstract]

2022 Aug;20(8):1900-1909. PMID: 35622056
BMC Cancer

Eltrombopag inhibits the proliferation of Ewing sarcoma cells via iron chelation and impaired DNA replication. [Abstract]

2020 Nov 30;20(1):1171. PMID: 33256675
Viruses

Screening of an FDA-Approved Drug Library with a Two-Tier System Identifies an Entry Inhibitor of Severe Fever with Thrombocytopenia Syndrome Virus. [Abstract]

2019 Apr 25;11(4):385. PMID: 31027241
Eur J Clin Pharmacol

Relationship between CYP2C8, UGT1A1, and ABCG2 gene polymorphisms and the exposure, efficacy, and toxicity of eltrombopag in the treatment of refractory aplastic anemia. [Abstract]

2022 Oct;78(10):1657-1666. PMID: 35922716
J Pharm Biomed Anal

Simultaneous analysis of avatrombopag, eltrombopag, and hetrombopag in human plasma by UPLC-MS/MS for therapeutic drug monitoring. [Abstract]

2023 Oct 25:235:115683. PMID: 37647792
Curr Microbiol

Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. [Abstract]

2021 Apr;78(4):1159-1167. PMID: 33611618
Virology

Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]

2023 Aug:585:205-214. PMID: 37384967
bioRxiv

2026 Jan 21.
bioRxiv

2025 Sep 13.
Biomed Pharmacother

Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]

2025 Jun 20:189:118246. PMID: 40543162
bioRxiv

2025 March 03.

Solvant et solubilité

In Vitro:

DMSO : 8.33 mg/mL (18.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2600 mL

11.3002 mL

22.6004 mL

5 mM

0.4520 mL

2.2600 mL

4.5201 mL

10 mM

0.2260 mL

1.1300 mL

2.2600 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
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Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30. [Content Brief]

[2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93. [Content Brief]

[3]. Lee H, et al. Repurposing Eltrombopag for Multidrug Resistant Staphylococcus aureus Infections. Antibiotics (Basel). 2021 Nov 9;10(11):1372. [Content Brief]

[4]. Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21. [Content Brief]

[5]. Kurokawa T, et al. The Eltrombopag antitumor effect on hepatocellular carcinoma. Int J Oncol. 2015 Nov;47(5):1696-702. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2600 mL	11.3002 mL	22.6004 mL	56.5010 mL
	5 mM	0.4520 mL	2.2600 mL	4.5201 mL	11.3002 mL
	10 mM	0.2260 mL	1.1300 mL	2.2600 mL	5.6501 mL
	15 mM	0.1507 mL	0.7533 mL	1.5067 mL	3.7667 mL

Eltrombopag

24 Cited Publications

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Eltrombopag

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Apoptosis Compound Library

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Publications Citing Use of MedChemExpress (MCE) Eltrombopag

Activité biologique

Chemical Information

Publications (24)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Eltrombopag Related Classifications

HY-15306 Related Classifications