Navitoclax, also known as ABT-263 and ABT 263, is a potent, oral biologically active inhibitor of the Bcl-2 protein family, acting on Bcl-xL, Bcl-2 and Bcl-w, with Ki of ≤0.5 nM, respectively , ≤1 nM and ≤1 nM. Navitoclax has anti-tumor activity on a variety of cells, such as H146, H82, H889, H1963, and H1417, and causes tumor regression in the body. Moreover, Navitoclax can enhance the therapeutic effect of chemotherapy drugs.

(1) In vitro research

Establish a mammalian two-hybrid system in HeLa cells, incubate the cells with ABT-263 (0-500 nM), ABT-263 destroys the interaction between Bcl-2 family proteins, and ABT-263 inhibits VP16-Bcl-xS and Gal4 -Bcl-xL interaction, EC50 is about 50 nM. 

(2) In vivo research

In in vivo experiments, different doses of ABT-263 (25-100 mg/kg/d) were orally administered to transplanted tumor mice. ABT-263 showed a high inhibitory effect on SCLC and ALL, and 100 mg/kg ABT-263 caused rapid , Complete tumor regression.