VISTA-IN-4 (Compound B3) is an orally active inhibitor of the immune checkpoint protein VISTA, with a KD of 0.452 µM. It degrades VISTA in HepG2 cells with a degradation rate of 77% at a concentration of 5 µM. VISTA-IN-4 counteracts VISTA-mediated immune suppression, restoring T cell activity and promoting the release of cytokine IL-2. Additionally, it exhibits antitumor activity in CT26 xenograft mouse models and demonstrates favorable pharmacokinetic properties, with good oral serum exposure in SD rats, reflected by an AUC(0-t) of 412.9 mgh/mL.
Molekulargewicht:
388.48
Formel:
C24H25FN4
Target-Kategorie:
Others
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