Eltrombopag
Eltrombopag
CAS: 496775-61-2
Molecular Formula: C25H22N4O4
Eltrombopag - Names and Identifiers
| Name | Eltrombopag |
| Synonyms | Sb497115 Promacta Sb-497115 Eltrombopag Unii-S56D65xj9g Eltrombopag [inn] (E)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxybiphenyl-3-carboxylic acid (1,1'-Biphenyl)-3-carboxylic acid, 3'-((2Z)-(1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene)hydrazino)-2'-hydroxy- 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 |
| CAS | 496775-61-2 |
| EINECS | 610-469-9 |
| InChI | InChI=1/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22- |
Eltrombopag - Physico-chemical Properties
| Molecular Formula | C25H22N4O4 |
| Molar Mass | 442.47 |
| Density | 1.33 |
| Melting Point | 242-244°C |
| Boling Point | 656.8±65.0 °C(Predicted) |
| Solubility | 25°C: DMSO 89 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL |
| Appearance | Powder |
| Color | Orange |
| pKa | -1.26±0.40(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| Refractive Index | 1.666 |
| Use | An agonist of the thrombopoietin receptor |
| In vitro study | Half maximal effective concentration (EC50) of Eltrombopag in mouse BAF3 cells transfected with luciferase reporter gene containing STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR) regulation 0.27 μm. Eltrombopag activates receptors by binding specific amino acids within the transmembrane and transmembrane domains of metallic iron (I. e., Zn2) and TpoR. Immunoblotting with anti-phospho-stat5 antibody showed that Eltrombopag (30 μm) activated STAT5 in N2C-Tpo cells. After 2 days of incubation, proliferation was stimulated by Eltrombopag and BrdU assay was performed on BAF3/hTpoR cells with an EC50 of 0.03 μm. Eltrombopag also induces the differentiation of hematopoietic stem cells into megakaryocytic progenitor cells. Eltrombopag dose-dependently increased the differentiation of bone marrow CD34 cells into CD41 megakaryocytes with an EC50 of 0.1 μm. Eltrombopag inhibited the proliferation of N2C-Tpo cells and HEL92.1.7 cells with an IC50 of 20.7 μg/mL and 2.3 μg/mL, respectively. In human and mouse leukemia cells, Eltrombopag (20 μg/mL) resulted in reduced cell division rates, g (1) phase arrest of the cell cycle, and increased cell differentiation. In HL60 cells, Eltrombopag (5 μg/mL) showed significant differentiation signals, significantly changed the structure of nuclear contents, and increased the cytoplasmic/nuclear ratio. Eltrombopag (5 μg/mL) increased CD11b, consistent with premacrophage status in U937 cells, and caused an increase in CD11b in URE cells. In leukemia HL60 cells, Eltrombopag caused a dose-dependent reduction in intracellular free iron ions. |
| In vivo study | One week after the last dose of Eltrombopag (10 mg/kg daily), the number of blood cells increased approximately more than 2-fold in one chimpanzee and approximately 1.5-fold in the other two chimpanzees. Eltrombopag (1 mg/ml) prolongs the survival time of a mouse model of leukemia. |
Eltrombopag - Introduction
Eltrombopag is a small molecule, c-mpl (TpoR) receptor agonist, inhibiting hERG K channel tail current with IC50 of 0.69 μM.
Last Update：2022-10-16 17:25:28
Supplier List
Spot supply
Product Name: Eltrombopag Visit Supplier Webpage Request for quotationCAS: 496775-61-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Eltrombopag Visit Supplier Webpage Request for quotationCAS: 496775-61-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Eltrombopag Visit Supplier Webpage Request for quotationCAS: 496775-61-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Eltrombopag Visit Supplier Webpage Request for quotationCAS: 496775-61-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History