in vitro: BMS-387032 displays no activity against 190 additional kinases (IC50 >1000 nM). BMS-387032 arrests the cell cycle at G2/M; inhibits transcription, proliferation and colony formation, and induces apoptosis in RPMI-8226 multiple myeloma cells. BMS-387032 prevents tumor cell-induced VEGF secretion and in vitro angiogenesis. SNS-032 inhibits three dimensional capillary network formations of endothelial cells. SNS-032 completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, SNS-032 significantly prevents the production of VEGF in both cell lines, SNS-032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS-032 induces cell cycle arrest and apoptosis across multiple cell lines.

in vivo: SNS-032 prevents tumor cell-induced VEGF secretion in a tumor coculture model. SNS-032, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors.