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Purity: ≥98%
Eltrombopag (formerly SB-497115; SB 497115; SB497115; trade name PROMACTA), a member of the biarylhydrazone class, is a novel nonpeptide agonist of the thrombopoietin receptor (TpoR) approved for use in the treatment of chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP). Eltrombopag demonstrates an 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. 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.
| ln Vitro |
When luciferase reporter gene is transfected into mouse BAF3 cells, eltrombopag (0.002-50 μM; 4 h) exhibits activity [1]. Eltrombopag (30 μM; 120 min) has an impact on the way that p-N2C-Tpo STAT5 is activated in cells [1]. In megakaryocytes, eltrombopag (30 μM; 120 minutes) stimulates p-STAT5[1]. BAF3/hTpoR cell proliferation is stimulated by eltrombopag (0.1 nM-10 μM; 30 min) [1]. Eltrombopag (0.03-3 μM; 10 days) promotes CD34+ cells in the bone marrow to differentiate into CD41+ megakaryocytes [1]. N2C-Tpo cell apoptosis is impacted by eltrombopag (0-3 μM; 72 h)[1]. With a MIC50 of 0.3 mg/L, eltrombopag efficiently prevents the growth of pneumococci, but it is ineffective against Gram-negative bacteria [3]. Eltrombopag (0 -200 mg/L; 24 hours; HepG2 and Caco-2 cells) has a MIC50 of 1.5 mg/L, which is less effective than that of vancomycin (MIC50 of 1.2 mg/L), when used in combination. L[3]. In Huh7 cells, eltrombopag (0 or 10 μg/mL; 72 h) strongly promotes G0/G1 phase arrest [5]. On HCC cell lines, eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative action [5].
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| ln Vivo |
Chimpanzees can tolerate Eltrombopag Olamine (10 mg/kg) when given orally once day for five days [1]. Mean S is greatly decreased by elotrombopag Olamine (17.6 mg/kg; i.p.; once daily for two days). Mice's nasal infections with aureus numbers [3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Murine BAF3 cells Tested Concentrations: 0.002-50 μM Incubation Duration: 4 h Experimental Results: Effectively inhibited murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM. [1][1] Cell Types: N2C-Tpo cells and CD34+ Tested Concentrations: 30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34+ Incubation Duration: 120 min for N2C-Tpo cells; 30 min for CD34+ Experimental Results: Activated phospho-STAT5 and maximum signal intensity demonstrated 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 Types: BAF3/hTpoR cells Tested Concentrations: 0.1 nM-10 μM Incubation Duration: 2 days Experimental Results: Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM. Cell Differentiation Assay[1] Cell Types: CD34+ Tested Concentrations: 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM Incubation Duration: 10 days Experimental Results: Dose-dependently stimulated the differentiation from bone marrow CD34+ cells to CD |
| Animal Protocol |
Animal/Disease Models: Female chimpanzees[1]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 10 mg/kg one time/day; for 5 days Experimental Results: Appeared a goes up and then goes back tendency of platelet counts after treatment, and demonstrated no bad effects of hematology, coagulation, or clinical chemistry parameters on animal. Animal/Disease Models: 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] Doses: 17.6 mg/kg Route of Administration: IP; one time/day for 2 days Experimental Results: Dramatically decreased mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) lung) mice. |
| References |
[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.
[2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93. [3]. Lee H, et al. Repurposing Eltrombopag for Multidrug Resistant Staphylococcus aureus Infections. Antibiotics (Basel). 2021 Nov 9;10(11):1372. [4]. Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21. [5]. Kurokawa T, et al. The Eltrombopag antitumor effect on hepatocellular carcinoma. Int J Oncol. 2015 Nov;47(5):1696-702. |
| Molecular Formula |
C25H22N4O4
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| Molecular Weight |
442.47
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| Exact Mass |
442.16411
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| CAS # |
496775-61-2
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| Related CAS # |
Eltrombopag Olamine;496775-62-3;(E/Z)-Eltrombopag-13C4;1217230-31-3
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| 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
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| Chemical Name |
3-[2-[(2Z)-1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2-hydroxy-[1,1-biphenyl]-3-carboxylic acid
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| Synonyms |
Eltrombopag; SB497115; SB-497115; SB 497115; SB497115GR; trade name: PROMACTA
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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