BRD9500

1630760-75-6

291.32

10 mM in DMSO

Metabolic Enzyme/Protease

BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC₅₀s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity^[1]. IC50 & Target: IC50: 10 nM (PDE3A), 27 nM (PDE3B)^[1] In Vitro: BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12^[1].
BRD9500 exhibits an EC₅₀ of 1 nM for SK-MEL-3 melanoma cell line viability^[1].
BRD9500 exhibits an EC₅₀ of 1.6 nM for HeLa viability^[1].
BRD9500 (10 uM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells^[1]. In Vivo: BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice^[1].
BRD9500 shows high plasma levels in mice after iv (1 mg/kg) as well as po (2 mg/kg) dosing over eight hours making it a valuable candidate for in vivo xenograft testing^[1].