tcsc0014 ABT-737

ABT-737 is a selective and BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor with EC₅₀s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

IC50 & Target: EC50: 78.7 nM (Bcl-xL), 30.3 nM (Bcl-2), 197.8 nM (Bcl-w)^[3]

In Vitro: ABT-737 and ATO inhibits proliferation and induces apoptosis in SGC-7901 and MGC-803 cells in concentration- and time-dependent manner, and shows a synergistic effect. ABT-737 disturbs the binding of B cell lymphoma (Bcl)-2 homologous antagonist killer and Bcl-extra large^[1]. ABT-737 induces a BAX/BAK-dependent impairment of maximal O₂ consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O₂ consumption rate in B-cell lymphoma cells^[2]. ABT-737 induces apoptosis and synergizes with chemotherapy,and disrups BCL-2/BAX heterodimerization and induces BAX conformational change in AML cells^[3].

In Vivo: ABT-737 (50 mg/kg, i.p.) and ATO significantly suppress SGC-7901 xenograft growth, synergistically inhibit tumour growth and induce apoptosis in vivo^[1]. ABT-737 suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively^[3].