Rafutrombopag
Based on 1 Customer Validation
Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease.
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- Pureza: 95.29%
- No. CAS: 2600513-51-5
- Fòrmula: C25H22N4O5
- Peso molecular:458.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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CDK4 |
CDK6 |
PI3K |
Rafutrombopag (0.01-1000 nM, 0-7 days) stimulates intracellular TPO signalling pathways and promotes 32D-MPL (EC50 = 0.4 nM) and BaF3/h TPOP ( EC50 = 1.2 nM) cell proliferation in a TPOR-dependent manner[1][2].
Rafutrombopag (0.01-10 μM, 0-10 days) promotes proliferation (EC50 = 2.3 nM) and differentiation of human cord blood-derived CD34+ cells[1][2].
Rafutrombopag (0-3 μM, 24-72 h) normalizes cell-cycle progression and prevents apoptosis in 32D-MPL cells and rat cardiac myocytes[1].
Rafutrombopag (0.01-1000 nM, 30 min-72 h) interacts specifically with TPOR and exerts an additive agonistic effect with rhTPO[1].
Rafutrombopag (0.3-3 μM, 12 h) enhances the beneficial effects of human UCB MNCs in increasing the survival of injured cardiomyocytes during free oxygen radical stress by enhancing human UCB MNCs viability and increasing the secretion of paracrine factors[2].
Rafutrombopag (3-30 μM) has anti-inflammatory activity and significantly reduces the production of NO and TNF-a in LPS (HY-D1056) stimulated macrophage RAW264.7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:32D-MPL cells
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Concentration:0.3.1 and 3 nM
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Incubation Time:24 h
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Result:Caused cells to re-enter the cell cycle, increasing the proportion of cells in G2 and S phases and decreasing the proportion of cells in G1 phase.
Reversed the decrease in G1-phase-related proteins, including p-RB, Cyclin D and CDK4/6, induced by cytokine withdrawal.
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Cell Line:32D-MPL cells
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Concentration:0.3.1 and 3 nM
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Incubation Time:72 h
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Result:Reduced the apoptosis effect.
Increased expression of the antiapoptotic family members BCL-XL and MCL-1, and decreased expression of proapoptotic BAK.
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Cell Line:32D-MPL cells
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Concentration:0.1, 1, 3, 10, 30, 100 nM
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Incubation Time:0, 0.5, 1, 2, 4, 8, 12, 24h
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Result:Induced phosphorylation of the major components of TPO‐mediated signalling, including STAT3, STAT5, ERK1/2, and AKT.
Stimulated the phosphorylation of these TPOR downstream effectors in a concentration-dependent manner.
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Cell Line:32D-MPL cells
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Concentration:0.3.1 and 3 μM
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Incubation Time:12 h
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Result:Increased myocyte viability by 20.3%, 43.7% and 46.8% at 0.3, 1 and 3 μM, respectively.
Showed weak antioxidant activity, and increased the myocyte viability by 15.7%.
Rafutrombopag (18 mg/kg, p.o., once daily for 12 days) significantly stimulates proliferation and prevents apoptosis of 32D-MPL cells in hollow fibres in a time-dependent manner in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:32D-MPL cell-containing hollow fibres assay established in mice[1]
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Dosage:18 mg/kg
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Administration:Oral administration (p.o.), once daily for 12 days
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Result:Significantly stimulated proliferation and prevented apoptosis of 32D-MPL cells in hollow fibres in a time-dependent manner.
Reached the number of 32D-MPL cells a maximum after 3 days and then decreased within 12 days.
Had no effect on the counts of white blood cells, reticulocytes, or platelets in the peripheral blood.
Chemical Information
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No. CAS 2600513-51-5
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Appearance Solid
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Peso molecular 458.47
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Fòrmula C25H22N4O5
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Color Brown to red
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SMILES
O=C1N(N=C(/C1=N/NC2=C(C(C3=CC=C(C(O)=O)O3)=CC=C2)O)C)C4=CC=C(CCCC5)C5=C4
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Synonyms
Hetrombopag; SHR-8735
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 33.33 mg/mL (72.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Xie C, et al. Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist. J Cell Mol Med. 2018 Nov;22(11):5367-5377. [Content Brief]
[2]. Zhou N, et al. Hetrombopag, a Thrombopoietin Receptor Agonist, Protects Cardiomyocyte Survival from Oxidative Stress Damage as an Enhancer of Stem Cells. Cardiovasc Drugs Ther. 2016 Dec;30(6):567-577. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1812 mL | 10.9058 mL | 21.8117 mL | 54.5292 mL |
| 5 mM | 0.4362 mL | 2.1812 mL | 4.3623 mL | 10.9058 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1812 mL | 5.4529 mL | |
| 15 mM | 0.1454 mL | 0.7271 mL | 1.4541 mL | 3.6353 mL | |
| 20 mM | 0.1091 mL | 0.5453 mL | 1.0906 mL | 2.7265 mL | |
| 25 mM | 0.0872 mL | 0.4362 mL | 0.8725 mL | 2.1812 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7271 mL | 1.8176 mL | |
| 40 mM | 0.0545 mL | 0.2726 mL | 0.5453 mL | 1.3632 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0906 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3635 mL | 0.9088 mL |
Rafutrombopag Related Classifications
HY-145589 Related Classifications
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