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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. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A. 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. 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.
| Molecular Weight | 649.65 |
| Formula | C29H34Cl2N6O3S2 |
| CAS Number | 570406-98-3 |
| Solubility (25°C) | DMSO 8 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] No authors listed. Avatrombopag
[2] Anthony Markham. Drugs. Avatrombopag: A Review in Thrombocytopenia
[4] Matt Shirley. Drugs. Avatrombopag: First Global Approval
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