Cabazitaxel

半合成紫杉烷；通过减少微管蛋白组装的滞后时间（LT50=100nM）和体外冷诱导微管解聚的速率（IC50=100-250nM）来稳定微管组装；抑制P388、HL-60、Calc18和KB细胞（IC50s=4-41nM）以及这些细胞系的P糖蛋白表达、药物耐药版本（IC50s=16-414nM）的增殖；剂量依赖性地降低对多西他赛敏感的N87人胃癌和对多西他赛耐药的UISOBCA-1乳腺癌小鼠异种移植模型中的肿瘤生长。A semisynthetic taxane; stabilizes microtubule assembly by reducing lag time for tubulin assembly (LT50 = 100 nM) and the rate of cold-induced microtubule depolymerization (IC50 = 100-250 nM) in vitro; inhibits proliferation of P388, HL-60, Calc18, and KB cells (IC50s = 4-41 nM), as well as P-glycoprotein-expressing, drug-resistant versions of these cell lines (IC50s = 16-414 nM); dose-dependently reduces tumor growth in docetaxel-susceptible N87 human gastric carcinoma and docetaxel-resistant UISO BCA-1 breast cancer mouse xenograft models.