Discovery of TK-642 as a highly potent, selective, orally bioavailable pyrazolopyrazine-based allosteric SHP2 inhibitor

• Main Authors: Kai Tang (Author), Shu Wang (Author), Siqi Feng (Author), Xinyu Yang (Author), Yueyang Guo (Author), Xiangli Ren (Author), Linyue Bai (Author), Bin Yu (Author), Hong-Min Liu (Author), Yihui Song (Author)
• Format: Book
• Published: Elsevier, 2024-08-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a promising therapeutic target for cancer therapy. In this work, we presented the structure-guided design of 5,6-fused bicyclic allosteric SHP2 inhibitors, leading to the identification of pyrazolopyrazine-based TK-642 as a highly po...