CBPD-409 is an orally active CBP/p300 degrader with a DC50 of 0.2–0.4 nM. It exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP, and 22Rv1, with an IC50 of 1.2–2.0 nM. Additionally, CBPD-409 shows antitumor activity.

CBPD-409 (0.01-10 nM) inhibits AR signaling and c-Myc expression in prostate cancer cell lines VCaP, LNCaP, and 22Rv1.

CBPD-409 demonstrates pharmacokinetic properties in an ICR mouse model with a clearance rate (CL) of 1.7 mL/min/kg, and a half-life (T 1/2) of 2.8 hours (intravenous injection) and 2.6 hours (oral administration). The maximum plasma concentration (C max) reaches 2494 ng/mL, with an oral bioavailability (F) of 50%. Administered orally at 0.3-1 mg/kg once daily for 5 weeks, CBPD-409 exhibits antitumor activity against VCaP prostate cancer, achieving a tumor growth inhibition rate (TGI) of 73-87% without significant toxicity in the VCaP xenograft mouse model.