| CAS |
No.114977-28-5 |
| 中文名称 |
多西他赛(10mM in DMSO,无菌） |
| 英文名称 |
Docetaxel(10mM in DMSO，Sterile） |
| 分子式 |
C43H53NO14 |
| 分子量 |
807.88 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Microtubule/Tubulin |
| 通路 |
Cytoskeleton |
| 背景说明 |
Docetaxel是一种微管解聚 (microtubule depolymerization) 抑制剂， 能减弱 bcl-2 和 bcl-xL 基因表达的影响。 |
| 生物活性 |
Docetaxel (RP-56976) is a microtubule?depolymerization inhibitor， with an IC50 of 0.2 μM. Docetaxel attenuates the effects of?bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity.[1-4] |
| In Vitro |
Docetaxel (RP-56976) 和葡磷酰胺 (GLU) 的单一和联合处理以剂量依赖的方式影响细胞活力。GLU在PC-3和LNCaP细胞中的IC50分别为70±4 μM和86.8±8 μM。同时，在 PC-3 和 LNCaP 细胞中，单用 Docetaxel 的 IC50 分别为 3.08±0.4 nM 和 1.46±0.2 nM GLU与 Docetaxel 联合处理可协同细胞毒性，PC-3 和 LNCaP 细胞的 IC50 值分别降低至2.7±0.1 nM和0.75±0.3 nM[1]。 Docetaxel 对 NCI-H460 的 IC50 在24小时为116 nM，在72小时为30 nM。根据 DTP 数据搜索中报告的数据，NCI-60 细胞板对 Docetaxel 的平均 IC50 为 14-34 nM[2]. |
| In Vivo |
在雌性小鼠中，光照后 14 小时 (HALO) 组中 Docetaxel (RP-56976) 诱导的肠细胞凋亡明显大于 2-HALO 组。Bax 表达在 2-HALO 组中被 Docetaxel 显著升高，但在 14-HALO 组中没有。另一方面，Docetaxel 在 14-HALO 组中显著升高了裂解的 Caspase-3 表达，但在 2-HALO 组中没有。Wee1 和磷酸化 CKD1 的表达在 Docetaxel 给药后在 14 HALO 时显著升高，但在 2 HALO 时没有。此外，Docetaxel 显著降低 14-HALO 组中的存活蛋白表达，但不降低 2-HALO 组中的存活蛋白表达。Docetaxel 处理14-HALO组 survivin 表达水平明显低于药物处理2-HALO组[3]。胡椒碱 (PIP) 通过静脉给药以 3.5 mg/kg 推注并以 35 mg/kg 和 3.5 mg/kg 口服给药，而 Docetaxel (DOX) 以 7 mg/kg 静脉内给药至 Sprague-Daley 大鼠。在 Sprague-Dawley 大鼠中通过口服给药 35 mg/kg 的 PIP 和通过静脉推注给药 7 mg/kg 的 Docetaxel 共同给药。PIP 和 Docetaxel 的联合使用导致它们体内暴露的协同增加[4]。 |
| 细胞实验 |
Single-drug concentration-response curves are assessed. Seeding is done at a density of 2，000 cells/well for PC-3 and LNCaP， in 96-well plates. Cells are treated with each single drug and their combination for 72 h at different drug concentrations. Docetaxel is used at concentrations of 0.1-1，000 nM. GLU is used at concentrations of 0.1-300 μm. Cytotoxicity is assessed at the end of drug exposure using SRB assay. Following 72 h exposure the cells are fixed with 10% trichloroacetic acid (150 μL) for 1 h at 4°C. Then， cells are stained for 10 min at room temperature with 0.4% SRB dissolved in 1% acetic acid. The plates are then air dried for 24 h and the dye is made soluble with 150 μL Tris (10 mM， PH 7.4) for 5 min on a shaker at 1，600 rpm. Absorbance is then measured at 545 nM using microplate reader. Results are expressed as the relative percentage of absorbance compared to control[1]. |
| 动物实验 |
Mice[3] Five-week-old male Balb/c mice are used. Docetaxel (0， 10， 20， 30， 40， 60， and 80 mg/kg per week) is given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of Docetaxel causes body weight loss in mice， 20 mg/kg per week of Docetaxel is judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) is given to mice once a week for 3 weeks at one of the following different points (2， 10， 14， or 22 HALO). Seventy-two hours after the final dosing of the agent， the intestinal mucosa of the small intestine (proximal 8 cm) is removed， fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution)， and embedded in paraffin blocks， and sections of 5 μm are put on glass slides. Apoptosis is detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method， using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit. Rats[4] Male Sprague-Dawley rats with body weight between 230-250 g and age between 6-7 weeks are used. About 25 SD rats are divided into five groups receiving Docetaxel (7 mg/kg， i.v.)， PIP (35 mg/kg， p.o.) and their combined administration (DOX+PIP) as well as PIP (3.5 mg/kg， p.o.) and PIP (3.5 mg/kg， i.v.). A day before the drug administrations， the rats are anesthetized. Right jugular vein is cannulated with a polyethylene tubing (0.5 mm ID， 1 mm) for blood collection. |
| 数据来源文献 |
[1]. Attia RT， et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168.
[2]. Che CL， et al. DNA microarray reveals different pathways responding to NSC 125973 and docetaxel in non-small cell lung cancer cell line. Int J Clin Exp Pathol. 2013 Jul 15;6(8):1538-48.
[3]. Obi-Ioka Y， et al. Involvement of Wee1 in the circadian rhythm dependent intestinal damage induced by docetaxel. J Pharmacol Exp Ther. 2013 Oct;347(1):242-8.
[4]. Li C， et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号