产品说明书
Cabazitaxel
 |
同义名 : | 卡巴他塞 ;XRP6258;RPR-116258A;dimethoxydocetaxel US brand name: Jevtana.;axoid XRP6258;TXD 258;taxoid XRP6258 |
| CAS号 : | 183133-96-2 | |
| 货号 : | A209461 | |
| 分子式 : | C45H57NO14 | |
| 纯度 : | 98% | |
| 分子量 : | 835.932 | |
| MDL号 : | - | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(125.61 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor[1]. Cabazitaxel can bound to unfractionated microtubules with KD 7.4 μM (measured by [14C]-labled binding stoichiometries). Cabazitaxel is used as a microtubule-targeted cancer chemotherapeutic agent for treatment of metastatic castrationresistant prostate cancer after failure of docetaxel treatment. Compared with docetaxel, cabazitaxel can suppress microtubule dynamic instability significantly more potently in the presence of βIII-tubulin than in its absence. This was supported by the study of βIIItubulin-deleted microtubule assembly experiment orβIII-tubulin-knockdown MCF7 cells. Also, it was found that mitotic arrest IC50 for cabazitaxel was significantly more potent in control-transfected cells (8 nM) than in βIII-tubulin- knockdown cells (18 nM, a 2.3-fold difference). Thus, The selective potency of cabazitaxel on βIII-tubulin-containing level may explain the superior anti-tumor efficacy of cabazitaxe in tumors overexpressing βIII-tubulin [a]. Specifically, cabazitaxel has the ability to cross the blood–brain barrier[2]. Cabazitaxel is approved for use in combination with prednisone for treatment of metastatic hormone refractory prostate cancer previously treated with a docetaxel-containing regimen (see in FDA net). | ||
| 作用机制 | Cabazitaxel can bind and stabilize microtubules and suppress microtubule dynamic instability significantly more potently in the presence of βIII-tubulin than in its absence[3]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human A431 cells | Growth inhibition assay | Growth inhibition of human A431 cells by MTT assay, IC50=1.48 nM | 24405702 | ||
| human A549 cells | Growth inhibition assay | Growth inhibition of human A549 cells by MTT assay, IC50=1.48 nM | 24405702 | ||
| human DU145 cells | Growth inhibition assay | Growth inhibition of human DU145 cells by MTT assay, IC50=1.43 nM | 24405702 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03419442 | - | Not yet recruiting | February 28, 2019 | United States, New Jersey ... 展开 >> US database Not yet recruiting Whippany, New Jersey, United States, 07981 收起 << | |
| NCT01379339 | Squamous Cell Carcinoma of the... 展开 >> Head and Neck 收起 << | Phase 1 | Completed | - | United States, New York ... 展开 >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 收起 << |
| NCT01447225 | Solid Tumors | Phase 1 | Completed | - | United States, Indiana ... 展开 >> Lafayette, Indiana, United States, 47905 United States, New York Buffalo, New York, United States, 14263 United States, Ohio Cincinnati, Ohio, United States, 45267 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19111 France Villejuif, France 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.20mL 0.24mL 0.12mL |
5.98mL 1.20mL 0.60mL |
11.96mL 2.39mL 1.20mL |
| 参考文献 |
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