Navitoclax | CAS:923564-51-6

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Name:Navitoclax; ABT-263
Cat. No. :CS-0013
CAS No. :923564-51-6
Formula:C47H55ClF3N5O6S3
M. Wt. : 974.61
Solubility:10 mM in DMSO

Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki L, Bcl-2 and Bcl-w.IC50 & Target: Ki: L), 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].

Ackler S, et al. Navitoclax (ABT 263) and Bendamustine±Rituximab Induce Enhanced Killing of Non-Hodgkin's Lymphoma Tumors in Vivo. Br J Pharmacol. 2012 Oct;167(4):881-891. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189.