References: |
BXI-72 (NSC334072) is a potent, selective small molecule Bcl-XL inhibitor that targets the BH3 domain of Bcl-XL (Kd=0.9 nM); displays very low binding affinities with Bcl2 (Ki=283 nM), Mcl-1, Bcl-w and Bfl-1/A1 (Ki>1500 nM); potently suppresses lung cancer cell growth (H1299=0.49 uM, A549 IC50=0.68 uM), displays relatively selective cytotoxicity against lung cancer cells compared to normal human bronchial epithelial cells; caunses disruption of Bcl-XL/Bak or Bcl-XL/Bax interaction, oligomerization of Bak, and cytochrome c release from mitochondria in cells, BXI-72 exhibits more potent efficacy against human lung cancer than ABT-737 but less degree in platelet reduction in vivo. |