Kolb E Anders, Gorlick Richard, Keir Stephen T, Maris John M, Kang Min H, Reynolds C Patrick, Lock Richard B, Carol Hernan, Wu Jianrong, Kurmasheva Raushan T, Houghton Peter J, Smith Malcolm A
Nemours/A.I. duPont Hospital for Children, Wilmington, Delaware.
Pediatr Blood Cancer. 2015 Jun;62(6):1106-9. doi: 10.1002/pbc.25329. Epub 2014 Nov 18.
BAL101553 is a highly water soluble prodrug of BAL27862 that arrests tumor cell proliferation and induces cell death in cancer cells through disruption of the microtubule network. In vitro BAL27862 demonstrated potent activity, with the median relative IC50 (rIC50 ) of 13.8 nM (range 5.4-25.2 nM). The in vitro activity of BAL27862 against the PPTP cell lines is distinctive from that previously described for vincristine. BAL101553 induced significant differences in EFS distribution compared to control in 16 of 30 (53%) solid tumor xenografts and in two of four (67%) of the evaluable ALL xenografts. No objective responses were observed.
BAL101553是BAL27862的一种高度水溶性前药，它通过破坏微管网络来阻止肿瘤细胞增殖并诱导癌细胞死亡。在体外，BAL27862表现出强大的活性，中位相对半数抑制浓度（rIC50）为13.8纳摩尔（范围为5.4 - 25.2纳摩尔）。BAL27862对PPTP细胞系的体外活性与先前描述的长春新碱不同。与对照组相比，BAL101553在30个实体瘤异种移植模型中的16个（53%）以及4个可评估的急性淋巴细胞白血病异种移植模型中的2个（67%）中诱导了无进展生存期分布的显著差异。未观察到客观缓解。
