Eltrombopag (Synonyms: SB 497115) |
Katalog-Nr.GC12513
One-Click Copy Product Info
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Eltrombopag (SB-497115) ist ein oral aktiver Nicht-Peptid-Agonist des Thrombopoietin-Rezeptors.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 496775-61-2
Sample solution is provided at 25 µL, 10mM.
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Eltrombopag is a non-peptide thrombopoietin receptor (TPO-R) specific agonist with an EC₅₀ of 0.19µM for TPO-R[1]. Eltrombopag mimics the biological function of natural thrombopoietin by activating the TPO-R signaling pathway and is primarily used in the treatment of immune thrombocytopenia and chemotherapy-induced thrombocytopenia. Additionally, Eltrombopag also has an inhibitory effect on the hERG potassium channel [2].
In in vitro cultures of normal CD34+ cells, Eltrombopag (3µg/mL; 4h) can bypass the inhibitory effect of IFN-γ on TPO intracellular signaling in human hematopoietic stem cells[3]. In MEF cells, Eltrombopag (10μM; 6.5h) inhibited STS-induced, caspase-3/7 activity-mediated apoptosis in MEF cells expressing only BAX, but had no effect on MEF cells expressing only BAK [4]. In mouse embryonic fibroblasts, Eltrombopag (0–30μM; 24h) can bind to the BAK α4/α6/α7 groove to initiate BAK activation, inducing apoptosis that is dependent on BAK but not BAX [5].
In murine transplantation models of leukemia，Eltrombopag (0.4-1.0mg/mL; po; 50d) treatment significantly improved survival in these mice, and engrafted leukemia cells in Eltrombopag -treated mice showed increased CD11b and CD14 expression[6]. In a mouse model of immune-mediated bone marrow failure, Eltrombopag（20μg/g/d; ip; 10d） significantly downregulated cytokines associated with Th1 immune responses and upregulated cytokines associated with Th2 immune responses[7].
References:
[1]. Subbarayan R, Srinivasan D, Sadullah Usmani S, et al. Molecular insights on Eltrombopag: potential mitogen stimulants, angiogenesis, and therapeutic radioprotectant through TPO-R activation[J]. Platelets, 2024, 35(1): 2359028.
[2]. Pathak S, Roth M, Verma A, et al. Eltrombopag for the treatment of thrombocytopenia in patients with malignant and non-malignant hematologic disorders[J]. Expert opinion on drug metabolism & toxicology, 2013, 9(12): 1667-1675.
[3]. Alvarado L J, Huntsman H D, Cheng H, et al. Eltrombopag maintains human hematopoietic stem and progenitor cells under inflammatory conditions mediated by IFN-γ[J]. Blood, The Journal of the American Society of Hematology, 2019, 133(19): 2043-2055.
[4]. Spitz A Z, Zacharioudakis E, Reyna D E, et al. Eltrombopag directly inhibits BAX and prevents cell death[J]. Nature communications, 2021, 12(1): 1134.
[5]. Chen M, Hu L, Bao X, et al. Eltrombopag directly activates BAK and induces apoptosis[J]. Cell Death & Disease, 2023, 14(7): 394.
[6]. Roth M, Will B, Simkin G, et al. Eltrombopag inhibits the proliferation of leukemia cells via reduction of intracellular iron and induction of differentiation[J]. Blood, The Journal of the American Society of Hematology, 2012, 120(2): 386-394.
[]. Ding S, Liang X, Zhang T, et al. The effectiveness of rapamycin combined with Eltrombopag in murine models of immune‐mediated bone marrow failure[J]. Journal of Immunology Research, 2020, 2020(1): 1798795.
| Cell experiment [1]: | |
Cell lines | HL60 cells and URE cells |
Preparation Method | HL60 cells and URE cells were incubated with increasing concentrations of Eltrombopag for 72 hours. |
Reaction Conditions | 0.1-20μM; 72h |
Applications | Eltrombopag leads to a decreased cell division rate and a block in the G1 phase of the cell cycle in human and murine leukemia cells. |
| Animal experiment [1]: | |
Animal models | Murine transplantation models of leukemia |
Preparation Method | Ten million HL60 cells were IV injected into NSG mice via the tail vein and mice were treated starting at day +3 with 1.0mg/mL of Eltrombopag in the drinking water or with untreated drinking water. |
Dosage form | 0.4-1.0mg/mL; po; 50d |
Applications | Eltrombopag treatment significantly improved survival in these mice, and engrafted leukemia cells in Eltrombopag-treated mice showed increased CD11b and CD14 expression. |
References: | |
| Cas No. | 496775-61-2 | SDF | |
| Überlieferungen | SB 497115 | ||
| Chemical Name | 3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid | ||
| Canonical SMILES | CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)NN=C3C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C | ||
| Formula | C25H22N4O4 | M.Wt | 442.47 |
| Löslichkeit | ≥ 13.2mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.26 mL | 11.3002 mL | 22.6004 mL |
| 5 mM | 452 μL | 2.26 mL | 4.5201 mL |
| 10 mM | 226 μL | 1.13 mL | 2.26 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)