AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.
IC50&Target
A2aR/A2bR
体外研究
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 AB928. Multiplexed gene expression profiling using NanoString identified a cassette of 39 genes that are regulated by adenosine during moDC differentiation. AB928 shows rescue of these gene expression changes.
体内研究
Concurrent treatment with AB928 and chemotherapy results in significantly reduced tumor volume in vivo using AT3-OVA tumors; Similar results are observed for the combination of AB928 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. AB928 increases the antitumor immune response leading to suppressed tumor growth and increased immune cell infiltration in mouse syngeneic tumors.
分子式
C23H22N8O
分子量
426.47
CAS号
2239273-34-6
运输条件
Room temperature in continental US; may vary elsewhere.