AK-1690 is a potent and selective STAT6 PROTAC degrader that induces degradation of STAT6 proteins in cells (DC50=1 nM) and depletes STAT6 proteins in mouse tissues, which can be used in cancer research.

IL-4-stimulated HEPG2 cells:0.88 nM

In HEPG2 and CCRF-CEM cells, AK-1690 efficiently degrades endogenous STAT6 (DC₅₀ = 3.2 nM, Dmax > 90%). In IL-4-stimulated HEPG2 cells, AK-1690 significantly suppresses expression of downstream genes (e.g., CCL26, SOCS1) with an IC₅₀ of 0.88 nM[1].

In a CCRF-CEM xenograft mouse model, oral administration of AK-1690 at 1, 3, and 10 mg/kg (once daily for 21 days) led to dose-dependent tumor growth inhibition. At 10 mg/kg, STAT6 degradation was significant, and tumor volume was notably reduced without observable weight loss or toxicity, indicating strong in vivo efficacy and tolerability[1].