Cabazitaxel

Cabazitaxel(XRP-6258); 卡巴他赛
CAS: 183133-96-2
Formula: C₄₅H₅₇NO₁₄                             
Molecular Weight:  835.93
Biological Activity: Cabazitaxel is a semi-synthetic derivative of toxal, a natural taxoid microtubule inhibitor. Cabazitaxel has been shown to have antitumor activity in vitro, and while it has a lower affinity for the ATP-dependent efflux pump, P-glycoprotein 1 (P-gp) relative to toxal or docetaxel, it has shown greater ability to penetrate the blood-brain barrier than either. In mice and rat models, uptake of cabazitaxel has been shown to increase at concentrations above 11 μM and saturation has been seen at 13 μM. This seems to suggest that P-gp may be essential to transport cabazitaxel across the blood-brain barrier at specific threshold concentrations.