ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

  title={ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.},
  author={Christin Tse and Alexander R. Shoemaker and Jessica Adickes and Mark G. Anderson and Jun Chen and Sha Jin and Eric F Johnson and Kennan C. Marsh and Michael J. Mitten and Paul M. Nimmer and Lisa Roberts and Stephen K. Tahir and Yu Xiao and Xiu-fen Yang and Haichao Zhang and Stephen W. Fesik and Saul H. Rosenberg and Steven W. Elmore},
  journal={Cancer research},
  volume={68 9},
Overexpression of the prosurvival Bcl-2 family members (Bcl-2, Bcl-xL, and Mcl-1) is commonly associated with tumor maintenance, progression, and chemoresistance. We previously reported the discovery of ABT-737, a potent, small-molecule Bcl-2 family protein inhibitor. A major limitation of ABT-737 is that it is not orally bioavailable, which would limit chronic single agent therapy and flexibility to dose in combination regimens. Here we report the biological properties of ABT-263, a potent… CONTINUE READING
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