Navitoclax

Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (K_i < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-x_L, Bcl-2 and Bcl-w. IC50 & Target: Ki: < 1 nM (Bcl-x_L), < 1 nM (Bcl-2), < 1 nM (Bcl-w) In Vitro: Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC₅₀ for all of the lines in the panel is 1.91 µM^[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation at all paclitaxel doses tested in both SK-OV-3 and IGROV-1 cell lines^[2]. In Vivo: Navitoclax (100 mg/kg/day, p.o.) also improves responses to bendamustine-rituximab (BR) in a subset of tumours in mice xenograft^[3].