sabutoclax

Description: Sabutoclax (BI-97C1), a derivative of apogossypolone, is a novel and potent pan-Bcl-2 inhibitor with IC50 of 0.31 uM, 0.32 uM, 0.20 uM and 0.62 uM for Bcl-xL, Bcl-2, Mcl-1 and Bfl-1, respectively. It showed a high binding affinity to Bcl-xL both in NMR binding assay and in ITC assay, with a Kd value of 0.11uM. Sabutoclax also showed better cell membrane permeability than other apogossypolone derivatives. In PC3 cells, sabutoclax inhibited cell growth with EC50 value of 0.13 uM. In human BP3 cell line, sabutoclax induced cell apoptosis with IC50 value of 0.049 uM. In mice bearing M2182 cancer xenografts, administration of sabutoclax significantly reduced the tumor size. At dose of 5 mg/kg, sabutoclax induced near complete tumor growth suppression.

References: J Med Chem. 2010 May 27; 53(10):4166-76.