Avatrombopag
Based on 5 publication(s) in Google Scholar
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
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- Pureté: 99.83%
- CAS No.: 570406-98-3
- Formule: C29H34Cl2N6O3S2
- Masse moléculaire:649.65
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Avatrombopag
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Activité biologique
EC50: 3.3 nM (TPO receptor)[1]
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Cell Line
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Type | Value | Description | References |
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| BaF3 | EC50 |
3.3 nM
Compound: Avatrombopag
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Induction of cell proliferation of mouse BaF3 cells expressing full-length human TPO receptor by WST-1/1-methoxy PMS assay
Induction of cell proliferation of mouse BaF3 cells expressing full-length human TPO receptor by WST-1/1-methoxy PMS assay
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[PMID: 36758304] |
| Caco-2 | CC50 |
20.86 μM
Compound: AVATROMBOPAG
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
5.71 μM
Compound: AVATROMBOPAG
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
Avatrombopag (E5501; AKR-501) specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did[1].
Avatrombopag (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as did rhTPO[1].
Avatrombopag promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent fashion. The EC50 is 25 nM for Avatrombopag and the maximum activity of Avatrombopag is similar to that of rhTPO[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:0.003 μM, 0.03 μM, 0.3 μM, 3 μM
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Incubation Time:
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Result:Increased the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion.
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Cell Line:Ba/F3 cells
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Concentration:0.003 μM, 0.03 μM, 0.3 μM, 3 μM
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Incubation Time:15 minutes
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Result:Induced tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice (transplanted with human FL CD34+cells)[1]
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Dosage:0.3, 1, and 3 mg/kg
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Administration:P.o.; daily for 14 days
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Result:Dose-dependently increased the number of human platelets, resulting in approximately a 2.7‐fold increase at 1 mg/kg/d and a 3.0-fold increase at 3 mg/kg/d on day 14 after the start of administration.
Chemical Information
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CAS No. 570406-98-3
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Appearance Solid
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Masse moléculaire 649.65
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Formule C29H34Cl2N6O3S2
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Color White to light yellow
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SMILES
O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O
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Synonyms
AKR-501; E5501; YM477
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
2023 Mar;615(7950):127-133. PMID: 36813966 -
J Clin Invest
Eltrombopag inhibits TET dioxygenase to contribute to hematopoietic stem cell expansion in aplastic anemia. [Abstract]2022 Feb 15;132(4):e149856. PMID: 35085104 -
Eur J Pharmacol
The immune thrombocytopenia therapeutic Avatrombopag alleviates osteoporosis by targeting NFATc1 signaling. [Abstract]2026 Jan 10:1010:178377. PMID: 41297758 -
J Thromb Haemost
2022 Aug;20(8):1900-1909. PMID: 35622056 -
Solvant et solubilité
DMSO : 8.33 mg/mL (12.82 mM; ultrasonic and warming and heat to 60°C; 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)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (477 KB)
- English - EN (477 KB)
- Français - FR (477 KB)
- Deutsch - DE (477 KB)
- Norwegian - NO (477 KB)
- Español - ES (477 KB)
- Swedish - SV (477 KB)
- Italian - IT (477 KB)
- Korean - KR (477 KB)
- Portuguese - PT (477 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009;82(4):247-254. [Content Brief]
[2]. Xu H, et al. Avatrombopag for the treatment of thrombocytopenia in patients with chronic liver disease. Expert Rev Clin Pharmacol. 2019 Sep;12(9):859-865. [Content Brief]
[3]. Nomoto M, et al. Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs. Br J Clin Pharmacol. 2018;84(5):952-960. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5393 mL | 7.6965 mL | 15.3929 mL | 38.4823 mL |
| 5 mM | 0.3079 mL | 1.5393 mL | 3.0786 mL | 7.6965 mL | |
| 10 mM | 0.1539 mL | 0.7696 mL | 1.5393 mL | 3.8482 mL |
Avatrombopag Related Classifications
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