Etrumadenant_product_DataBase

Bioactivity

Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities[1][2].

Target

A2aR/A2bR

Invitro

In human in vitro cell cultures, moDC differentiated in the presence of adenosine showed a decreased ability to stimulate IFN-γ secretion from allogenic CD4+ T-cells in a MLR. This suppression is significantly reversed by addition of Etrumadenant. Multiplexed gene expression profiling using NanoString identified a cassette of 39 genes that are regulated by adenosine during moDC differentiation. Etrumadenant shows rescue of these gene expression changes[2].

In Vivo

Concurrent treatment with Etrumadenant and chemotherapy results in significantly reduced tumor volume in vivo using AT3-OVA tumors; Similar results are observed for the combination of Etrumadenant and NSC 266046. AB928 is also capable of suppressing growth of B16-F10 tumors both as a single agent or in combination with α-PD-1 therapy. Etrumadenant increases the antitumor immune response leading to suppressed tumor growth and increased immune cell infiltration in mouse syngeneic tumors[2].

Name

Etrumadenant

CAS

2239273-34-6

Formula

C23H22N8O

Molar Mass

426.47

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Seitz L, et al. Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteers. Invest New Drugs. 2019 Aug;37(4):711-721. [2]. Daniel DiRenzo, et al. AB928, a dual antagonist of the A2aR and A2bR adenosine receptors, relieves adenosine-mediated immune suppression [abstract].

PeptideDB

Etrumadenant

CAS: 2239273-34-6 F: C23H22N8O W: 426.47