Network Version
Navitoclax Data Sheet
| Product Name: | Navitoclax |
 |
|---|---|---|
| CAS No.: | 923564-51-6 | |
| Cat. No.: | HY-10087 | |
| MWt: | 974.61 | |
| Formula: | C47H55ClF3N5O6S3 | |
| Purity : | >98% | |
| Solubility: | DMF : ≥ 100 mg/mL;DMSO : 75 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1]. IC50 & Target:Ki: < 1 nM (Bcl-xL), < 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 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]. | ||
1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com