keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Docetaxel (RP-56976) 是紫杉醇的半合成类似物,是一种微管解聚抑制剂 (IC50=0.2 μM)。Docetaxel 可以减弱 bcl-2 和 bcl-xL 基因表达的影响,具有诱导凋亡、抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 238 | 现货 | ||
10 mg | ¥ 335 | 现货 | ||
25 mg | ¥ 555 | 现货 | ||
50 mg | ¥ 822 | 现货 | ||
100 mg | ¥ 1,450 | 现货 | ||
200 mg | ¥ 2,070 | 现货 | ||
500 mg | ¥ 3,750 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 597 | 现货 |
产品描述 | Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity. |
靶点活性 | microtubule:0.2 μM |
体外活性 |
方法:人肺癌细胞 NCI-H460 用 Docetaxel (0.2-200 nmol/L) 处理 24-72 h,使用 MTS 方法检测细胞活力。 结果:NCI-H460 在 72 h 时对 Docetaxel 的 IC50 为 0.030 μmol/L,24 h 时为 0.116 μmol/L。[1] 方法:人前列腺癌细胞 PC-3、DU-145 和 LNCaP 用 Docetaxel (0.5-4 nM) 处理 48 h,使用 Flow Cytometry 检测细胞凋亡情况。 结果:高剂量 Docetaxel 处理显著增加了 Annexin V+ 凋亡细胞的比例。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Docetaxel (5-10 mg/kg) 和 PD-1 inhibitor (200 μg/只) 腹腔注射给携带小鼠前列腺癌肿瘤 RM-1 的 CB17 SCID 小鼠,每周五次,持续十天。 结果:PD-1 inhibitor 联合 Docetaxel 对小鼠前列腺癌具有协同作用,抑制了前列腺肿瘤的生长,提高了存活率并减少了不良反应。[3] 方法:为检测体内抗肿瘤活性,将 Docetaxel (7.5-15 mg/kg,瘤内注射 IT,每周两次,持续六周;或每周 20-40 mg/kg,静脉注射 IV) 给药给携带 HNSCC 肿瘤 HN30 或 HN12 的 C57BL/6 小鼠。 结果:IT Docetaxel 提高了整体存活率和无病生存率,并逆转了肿瘤生长。在同等剂量水平下,IT Docetaxel 的肿瘤峰值浓度比 IV 治疗高 26 倍,肿瘤暴露时间比 IV 治疗长 24 倍。[4] |
细胞实验 | NCI-H460 cells (4 × 10^3) were grown in 100 μl of DMEM medium containing serum per well in a 96-well plate. After 24 h, the cells were treated with docetaxel (0, 0.2, 0.63, 2, 6.3, 20, 63 and 200 nmol/L, respectively) for 72 h. Every treatment was triplicate in the same experiment. Then 20 μl of MTS was added to each well for 1 to 4 h at 37°C. After incubation, the absorbance was read at a wavelength of 490 nm according to the manufacturer's protocol. The IC50 calculation was performed with GraphPad Prism 5.0 software [2]. |
动物实验 | Docetaxel (0, 10, 20, 30, 40, 60, and 80 mg/kg per week) was given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of the drug caused body weight loss in mice, 20 mg/kg per week of docetaxel was judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) was 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) was removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5 mm were put on glass slides. Apoptosis was detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method, using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit. Specimens were dewaxed and immersed in phosphate-buffered saline for 5 minutes at room temperature, incubated with 20 mg/ml proteinase K for 15 minutes at room temperature, and then quenched of endogenous peroxidase in 2% hydrogen peroxide in phosphate-buffered saline. Terminal deoxynucleotidyl transferase enzyme was applied directly onto the specimens, which were then incubated at 37°C for 1 hour. The reaction was terminated by transferring the slides to stop/wash buffer for 10 minutes at room temperature, and then specimens were covered with peroxidase-conjugated anti-digoxigenin antibody and incubated for 30 minutes at room temperature. Specimens were then soaked in staining buffer containing 0.05% diaminobenzidine to achieve color development. Finally, the specimens were counterstained by immersion in Mayer's hematoxylin solution. Apoptotic cells were counted under a light microscope in a good longitudinal crypt section. Starting at the base of the crypt column, the TUNEL-positive cells were counted up to the 18th cell position in each crypt.One hundred crypt sections were scored in each animal, and a frequency of TUNELpositive cells per crypt was calculated. Dosing time-dependent influence of docetaxel on intestinal apoptosis was also examined in female Balb/c mice [5]. |
别名 | 多西他赛, NSC 628503, RP-56976, 多烯紫杉醇 |
分子量 | 807.88 |
分子式 | C43H53NO14 |
CAS No. | 114977-28-5 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 80.8 mg/mL (100 mM)
DMSO: 80.8 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.2378 mL | 6.189 mL | 12.3781 mL | 30.9452 mL |
5 mM | 0.2476 mL | 1.2378 mL | 2.4756 mL | 6.189 mL | |
10 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0945 mL | |
20 mM | 0.0619 mL | 0.3095 mL | 0.6189 mL | 1.5473 mL | |
50 mM | 0.0248 mL | 0.1238 mL | 0.2476 mL | 0.6189 mL | |
100 mM | 0.0124 mL | 0.0619 mL | 0.1238 mL | 0.3095 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Docetaxel 114977-28-5 Apoptosis Cytoskeletal Signaling Metabolism Microtubule Associated Endogenous Metabolite NSC628503 inhibit Inhibitor 多西他赛 NSC 628503 RP 56976 RP56976 NSC-628503 RP-56976 多烯紫杉醇 Microtubule/Tubulin inhibitor