1. Immunology/Inflammation
  2. Thrombopoietin Receptor
  3. Avatrombopag

Avatrombopag (Synonyms: AKR-501; E5501; YM477)

Cat. No.: HY-13463
Handling Instructions

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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Avatrombopag Chemical Structure

Avatrombopag Chemical Structure

CAS No. : 570406-98-3

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10 mM * 1 mL in DMSO USD 600 Ask For Quote & Lead Time
5 mg USD 420 Ask For Quote & Lead Time
10 mg USD 600 Ask For Quote & Lead Time
50 mg USD 1800 Ask For Quote & Lead Time
100 mg USD 2520 Ask For Quote & Lead Time

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Description

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[1][2][3].

IC50 & Target

EC50: 3.3 nM (TPO receptor)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cells
Concentration: 0.003 μM, 0.03 μM, 0.3 μM, 3 μM
Incubation Time:
Result: Increased the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells
Concentration: 0.003 μM, 0.03 μM, 0.3 μM, 3 μM
Incubation Time: 15 minutes
Result: Induced tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells.
In Vivo

Avatrombopag (0.3-3 mg/kg; p.o.; daily for 14 days) increases the number of human platelets in NOD/SCID mice transplanted with human FL CD34+ cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID mice (transplanted with human FL CD34+cells)[1]
Dosage: 0.3, 1, and 3 mg/kg
Administration: P.o.; daily for 14 days
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.
Molecular Weight

649.65

Formula

C₂₉H₃₄Cl₂N₆O₃S₂

CAS No.

570406-98-3

SMILES

O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (49.26 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5393 mL 7.6965 mL 15.3929 mL
5 mM 0.3079 mL 1.5393 mL 3.0786 mL
10 mM 0.1539 mL 0.7696 mL 1.5393 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

AvatrombopagAKR-501 E5501 YM477AKR501AKR 501E5501E 5501E-5501YM477YM 477YM-477Thrombopoietin ReceptormimicTPOmegakaryocytopoiesismegakaryocytesphosphorylationproliferationNOD/SCIDInhibitorinhibitorinhibit

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Avatrombopag
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