CPD-002 is an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR 2) that suppresses angiogenesis by inhibiting the VEGFR2/PI3K/AKT signaling pathway. Additionally, CPD-002 demonstrates anti-inflammatory properties and mitigates rheumatoid arthritis [1].

CPD-002 exhibits dose-dependent cytotoxicity on HUVEC and MH7A cells at concentrations ranging from 0-64 μM over 24-48 hours. It inhibits VEGF-induced migration and invasion of HUVEC cells by suppressing F-actin expression and the chemotactic response to chemokines released from MH7A cells at 0-8 μM for 24 hours. CPD-002 also demonstrates anti-inflammatory activity, inhibiting synovial angiogenesis by reducing the expression of inflammatory mediators such as TNF-α, IL-1β, IL-6, IL-8, MMP2, and MMP9 at concentrations of 0-8 μM. Additionally, at the same concentration range over 9 days, CPD-002 suppresses tube and sprout formation in ex vivo rat aortic ring assays. [1] Cell Viability Assay [1] Cell Line: HUVECs and MH7A Concentration: 0-64 μM Incubation Time: 24-48 h Result: Inhibited cell viability in a dose-dependent manner. Cell Migration Assay [1] Cell Line: HUVECs Concentration: 0-8 μM Incubation Time: 24 h Result: Inhibited HUVECs migration in a dose-dependent manner.

CPD-002 (15-60 mg/kg, administered via intraperitoneal injection once daily for 14 days) exhibits anti-arthritis and anti-angiogenesis activities in Sprague Dawley rats with adjuvant-induced arthritis (AIA) [1]. This treatment resulted in reduced paw swelling, decreased joint damage, and diminished synovial angiogenesis.