ErbB2/HER2 Degrader

PROTAC HER2 degrader-1 is a selective HER2 PROTAC degrader with a DC₅₀ of 69 nM. PROTAC HER2 degrader-1 induces ubiquitination and degradation of HER2 via the ubiquitin-proteasome system, thereby inhibiting the downstream PI3K/AKT/mTOR and RAS/RAF/MEK/ERK signaling pathways. PROTAC HER2 degrader-1 inhibits the proliferation of HER2-positive cancer cells, induces apoptosis and arrests the cell cycle. PROTAC HER2 degrader-1 suppresses the growth of HER2-positive xenografts. PROTAC HER2 degrader-1 can be used in HER2-positive cancer-related research.

COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer.

FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a K_D value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.

G3130 is a reversible HSP90 inhibitor with a K_d value of 280 nM for the N-terminal ATP-binding domain of purified human Hsp90α. G3130 binds to the adenine site via a multi-hydrogen bond network. G3130 induces the degradation of Hsp90 client protein Her-2 in breast cancer cells. G3130 activates Hsp70 promoter-driven luciferase expression in 293T cells. G3130 can be used in breast cancer-related research.