Navitoclax

923564-51-6

C47H55ClF3N5O6S3

DMSO : 75 mg/mL (76.95 mM; Need ultrasonic); DMF : >= 100 mg/mL (102.61 mM); H2O : < 0.1 mg/mL (insoluble)

Apoptosis

Navitoclax (ABT-263) is a potent and oral Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-x_L, Bcl-2 and Bcl-w, with a K_i of less than 1 nM. 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 uM^[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation in both SK-OV-3 and IGROV-1 cell lines^[2]. In Vivo: Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in vivo. As a single agent, 100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, the combination of Navitoclax and OSI-744 dosed daily for 21 consecutive days results in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice^[3].