Etrumadenant

MCE 国际站：Etrumadenant

产品活性：Etrumadenant (AB928) 是一种具有口服活性、选择性的腺苷受体 (A2aR/A2bR) 双拮抗剂。Etrumadenant 减轻腺苷介导的免疫抑制。Etrumadenant 具有免疫调节和抗肿瘤活性。

研究领域：GPCR/G Protein

作用靶点：Adenosine Receptor

In Vitro: 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.

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.

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