中文名称: 多西他赛 促销
英文名称: Docetaxel
CAS No: 114977-28-5
分子式: C43H53NO14
分子量: 807.88
EINEC: 628503
D10131 多西他赛 ≥98%(HPLC),分析标准品 (psaitong)
包装规格:
20mg in glass bottle
溶解性:
熔点:186-192°C 溶于DMSO (25mg/ml)和乙醇(25mg/ml)
产品描述:

基本信息

产品编号:D10131

产品名称:Docetaxel

CAS:

114977-28-5

 

储存条件

粉末

-20℃

四年

分子式:

C43H53NO14

溶于液体

-80℃(避光)

六个月

分子量:

807.88

-20℃(避光)

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

100mg/mL (123.78mM)

Ethanol

100mg/mL warmed with 50ºC water bath (123.78mM)

Water

Insoluble

体内(现配现用)

5% DMSO+30% PEG 300+5% Tween 80+ddH2O

2mg/mL

1mg/ml表示微溶或不溶。

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。

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
(Cell-free assay)

 

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:

 

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:

 

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. 

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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