Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

使用SF-295和U251人成胶质细胞瘤细胞系,产生原位和皮下鼠异种移植物. Cabazitaxel治疗导致大部分皮下植入的肿瘤完全消退.Cabazitaxel在其它相关模型中也有明显的抗肿瘤活性.Cabazitaxel在小鼠肿瘤异种移植模型 (结肠 C38 和 胰腺 P03)中,引起完全肿瘤消退.此外,Cabazitaxel在原位模型中导致10个U251肿瘤中的4个完全肿瘤消退.

Cabazitaxel的平均离体人血浆蛋白结合率为91.6％。Cabazitaxel会被迅速广泛地代谢成多种代谢产物。Cabazitaxel在多个鼠和人的抗性细胞系中都有活性。Cabazitaxel会提高大鼠肝细胞中CYP3A的酶活性。Cabazitaxel在3种结肠癌细胞株(HCT-116,HCT-8和 HT-29) 中显示出高抗肿瘤活性。用相对较低浓度的Cabazitaxel处理四天会产生明显的细胞毒性。

The cytotoxicity of CBX-loaded ANs and free Cabazitaxel (CBX) is evaluated with MTT assay. Cells are seeded onto a 96-well plate at a density of 3000 cells per well and cultured for 24 h. CBX-loaded ANs and free CBX are diluted to predetermined concentrations with PBS and added into each well. Blank AN, AN-ICG and free CBX solvent (a mixture of Tween-80 and anhydrous alcohol) are added as well to different final concentrations. The incubation continued for another 48 hours. 20 μL MTT solutions (5 mg/mL in PBS) are added into each well and cells are incubated for another 4 hours under 37°C. Subsequently the medium is removed and 150 μL dimethyl sulphoxide (DMSO) is added to dissolve the purple formazan salt crystals. Then the absorbance is measured by a microplate reader at 490 nm. The cells treated with medium are evaluated as controls.