ABT-263

Potent and selective Bcl-2 family inhibitor / BH3 domain mimetic which binds to Bcl-2, Bcl-xL and Bcl-w (Ki<1 nM) [1]. A useful tool compound which has shown interesting results in various cancer clinical trials [2]. Synergizes with deoxyglucose and other agents, inducing apoptosis in cancer cells in a xenograft mouse model [3]. A novel senolytic agent, inducing apoptosis preferentially in senescent cells in a cell type-restricted manner [4].

References:

1) Tse et al. (2008), ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor;  Cancer Res., 68 3421

2) Vogler et al. (2009), Bcl-2 inhibitors: small molecules with a big impact on cancer therapy;  Cell Death Differ., 16 360

3) Yamaguchi et al. (2011), Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy; PLoS ONE, 6(9) e24102

4) Zhu et al. (2016), Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors;  Aging Cell, 15 428