Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Adenosine A2b receptor antagonist
Product Description
Information
Etrumadenant (AB928) Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
Consistent with the ability of adenosine to suppress immune function, AB928 inhibits the ability of adenosine to suppress CD4 or CD8 T cell activation.
In vivo
Established AT-3-OVA tumors treated with AB928 alone has a small but significant decrease in their growth rate. Concurrent treatment with AB928 and chemotherapy results in significantly reduced tumor growth rates, when compared to chemotherapy alone.
1.Novitskiy SV, Ryzhov S, Zaynagetdinov R, Goldstein AE, Huang Y, Tikhomirov OY, Blackburn MR, Biaggioni I, Carbone DP, Feoktistov I et al.. (2008) Adenosine receptors in regulation of dendritic cell differentiation and function.. Blood, 112 (5):(1822-31). [PMID:18559975][10.1021/op500134e]
3.Seitz L, Jin L, Leleti M, Ashok D, Jeffrey J, Rieger A, Tiessen RG, Arold G, Tan JBL, Powers JP et al.. (2019) Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteers.. Invest New Drugs, 37 (4):(711-721). [PMID:30569245][10.1021/op500134e]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
L2320047
