中文名称: | 多西他赛 促销 | ||||
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英文名称: | Docetaxel | ||||
别名: | 多烯紫杉醇 Docetaxel | ||||
CAS No: | 114977-28-5 | 分子式: | C43H53NO14 | 分子量: | 807.88 |
CAS No: | 114977-28-5 | ||||
分子式: | C43H53NO14 | ||||
分子量: | 807.88 | ||||
MDL: | MFCD00800737 | EINEC: | 628503 | ||
EINEC: | 628503 |
基本信息
产品编号:D10131 |
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产品名称:Docetaxel |
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CAS: |
114977-28-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃(避光) |
六个月 |
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分子量: |
807.88 |
-20℃(避光) |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (123.78mM) |
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Ethanol |
100mg/mL warmed with 50ºC water bath (123.78mM) |
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Water |
Insoluble |
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体内(现配现用) |
5% DMSO+30% PEG 300+5% Tween 80+ddH2O |
2mg/mL |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.2378mL |
6.1890mL |
12.3781mL |
5mM |
0.2476mL |
1.2378mL |
2.4756mL |
10mM |
0.1238mL |
0.6189mL |
1.2378mL |
50mM |
0.0248mL |
0.1238mL |
0.2476mL |
生物活性
产品描述 |
一种紫杉类抗癌药物,它结合并稳定微管蛋白亚基,有丝分裂纺锤体的解聚,从而导致细胞周期阻滞和凋亡。 |
靶点/IC50 |
Microtubules |
体外研究 |
Docetaxel (RP-56976) and Glufosfamide (GLU) single and combined treatments affect the cells viability in a dose-dependent manner. The IC50 of GLU are 70±4µM and 86.8±8µM in PC-3 and LNCaP cells; respectively. While, the IC50 of Docetaxel alone is found to be 3.08±0.4nM and 1.46±0.2nM in PC-3 and LNCaP cells;respectively.The co-treatment of GLU with Docetaxel is found to synergize the cytotoxicity and the IC50 values are decreased to be 2.7±0.1nM and 0.75±0.3nM in PC-3 and LNCaP cells; respectively.IC50 of NCI-H460 to Docetaxel at 24 h is 116nM and at 72 h is 30nM. According to data reported in DTP Data Search, the mean IC50 of NCI-60 cell panel to Docetaxel is 14-34nM |
体内研究 |
In female mice, the Docetaxel (RP-56976)-induced intestinal apoptosis in the 14-hours after light on (HALO) group is significantly greater than that in the 2-HALO group. Bax expression is significantly elevated by Docetaxel in the 2-HALO group, but not in the 14-HALO group. On the other hand, cleaved Caspase-3 expression is significantly elevated by Docetaxel in the 14-HALO group, but not in the 2-HALO group. The expressions of Wee1 and phosphorylated CKD1 are significantly elevated after dosing of Docetaxel at 14 HALO, but not at 2 HALO. In addition,Docetaxel significantly reduces survivin expression in the 14-HALO group but not in the 2-HALO group. The survivin expression level in the Docetaxel-treated 14-HALO group is significantly smaller than that in the drug-treated 2-HALO group.Piperine (PIP) is administrated via intravenous bolus at 3.5mg/kg and via oral administration at 35mg/kg and 3.5mg/kg,while Docetaxel (DOX) is intravenously administrated at 7mg/kg to Sprague-Daley rats. The co administrations of PIP at 35mg/kg via oral administration and Docetaxel at 7mg/kg via intravenous bolus administration in Sprague-Dawley rats. The combination use of PIP and Docetaxel results in a synergic increase of both their in vivo exposure. |
推荐实验方法(仅供参考)
细胞实验: |
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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 72h at different drug concentrations. Docetaxel is used at concentrations of 0.1-1,000nM. GLU is used at concentrations of 0.1-300µm.Cytotoxicity is assessed at the end of drug exposure using SRB assay. Following 72 h exposure the cells are fixed with 10% trichloroacetic acid (150µL) for 1 h at 4℃. 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 24h and the dye is made soluble with 150µL Tris (10mM, PH 7.4) for 5 min on a shaker at 1,600 rpm. Absorbance is then measured at 545nM using microplate reader. Results are expressed as the relative percentage of absorbance compared to control. |
动物实验: |
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Mice Five-week-old male Balb/c mice are used. Docetaxel (0, 10, 20, 30, 40, 60, and 80mg/kg per week) is given once a week for 3 weeks for mice. Because more than 30mg/kg per week of Docetaxel causes body weight loss in mice, 20mg/kg per week of Docetaxel is judged to be the maximum nontoxic dose. Docetaxel (20mg/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 8cm) is removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5μm 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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )