The pyrazolopyrazine ring system is a very interesting class of heterocyclic compounds considered as important scaffolds for many effective bioactive agents with low toxicity, antioxidant, anticonvulsant, antiparasitic, anti-inflammatory, antiviral, antibacterial, anti- Fungal and analgesic activity.
Protein tyrosine phosphatase SHP2 mediates RAS-driven MAPK signaling and has emerged in recent years as a target of interest in oncology, both for treating with a single agent and in combination with a KRAS inhibitor. GDC-1971 (formerly RLY-1971) is a SHP2 inhibitor currently in clinical trials in combination with KRAS G12C inhibitor divarasib (GDC-6036) for the treatment of solid tumors driven by a KRAS G12C mutation.