TQ-3959 is an orally active BTKPROTAC degrader, with a DC50 of 14.6 nM. It exhibits antiproliferative activity against both wild-type BTK and BTK C481S mutant cell lines. TQ-3959 demonstrates tumor growth inhibition in female NOD-SCID mice with TMD-8 xenografts. This compound is applicable in the study of B-cell malignancies, such as lymphoma.

TQ-3959 demonstrates potent BTK degradation activity in OCI-Ly10 cells through HTRF experiments, with a DC₅₀ of 0.4 nM and a Dmax of 97.7%. Over 72 hours, TQ-3959 exhibits antiproliferative activity against OCI-Ly10 (BTK WT cells) (IC₅₀ = 0.08 nM), TMD-8 (BTK WT cells) (IC₅₀ = 1.0 nM), OCI-Ly10 (BTK C481S cells) (IC₅₀ = 0.2 nM), and TMD-8 (BTK C481S cells) (IC₅₀ = 0.6 nM).

TQ-3959, administered orally at doses of 7.5-30 mg/kg once daily for 20 days, has been shown to inhibit tumor growth in NOD-SCID mice xenografted with TMD-8.