WRG-28

WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC₅₀ of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice^[1][2]. In Vitro: WRG-28 (1, 2 µM; 4 h) blunts collagen I-mediated DDR2 tyrosine phosphorylation and (1 µM; 7 h) ERK activation as well as SNAIL1 protein stabilization in HEK293 cells (expressing DDR2) (IC₅₀=286 nM)^[1].
WRG-28 (1 μM; 48 h) blunts tumor cell invasion and migration by inhibiting DDR2 in BT549 and 4T1 breast cancer cells^[1].
WRG-28 (1 μM; 4 days) inhibits tumor-promoting effects of CAFs^[1].
WRG-28 (0.5, 1 μM; 4 h) maintains inhibitory action toward acquired DDR2 mutations that are resistant to TKIs^[1]. In Vivo: WRG-28 (10 mg/kg; i.v.; single) attenuates biochemical signaling of DDR2 in breast tumors in vivo^[1].
WRG-28 (10 mg/kg; i.v.; single daily for 7 days) reduces metastatic lung colonization of breast tumor cells^[1].
WRG-28 (10 mg/kg; i.v.; single daily for 21 days) decreases both the inflammatory reaction and joint destruction in mice with collagen antibody-induced arthritis (CAIA)^[2].