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Docetaxel

Docetaxel

产品编号 T1034   CAS 114977-28-5
别名: 多西他赛, NSC 628503, RP-56976, 多烯紫杉醇

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。

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Docetaxel Chemical Structure
Docetaxel, CAS 114977-28-5
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
其他形式的 Docetaxel:
产品目录号及名称: Docetaxel (T1034)
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纯度: 99.29%
纯度: 99.15%
纯度: 99.03%
纯度: 98.92%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
植物来源
结构类型
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

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 80.8 mg/mL (100 mM)

DMSO: 80.8 mg/mL (100 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Che CL, et al. DNA microarray reveals different pathways responding to paclitaxel and docetaxel in non-small cell lung cancer cell line. Int J Clin Exp Pathol. 2013 Jul 15;6(8):1538-48. 2. Yang C, et al. Effect of docetaxel on the regulation of proliferation and apoptosis of human prostate cancer cells. Mol Med Rep. 2019 May;19(5):3864-3870. 3. Zhou S, et al. PD-1 inhibitor combined with Docetaxel exerts synergistic anti-prostate cancer effect in mice by down-regulating the expression of PI3K/AKT/NFKB-P65/PD-L1 signaling pathway. Cancer Biomark. 2024 Jan 17. 4. Yoo GH, et al. An in vivo evaluation of docetaxel delivered intratumorally in head and neck squamous cell carcinoma. Arch Otolaryngol Head Neck Surg. 2005 May;131(5):418-29. 5. 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. 6. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168. 7. 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. 8. Chen Y, Li K, Gong D, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020: 153076. 9. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay[J]. Talanta. 2016, 161: 804-811. 10. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer[J]. Nature Communications. 2020, 11(1): 1-18.

文献引用

1. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer. Nature Communications. 2020, 11(1): 1-18. 2. Chen Y, Li K, Gong D I, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020, 216(9): 153076 3. Wavelet-Vermuse C, Odnokoz O, Xue Y, et al. CDC20-Mediated hnRNPU Ubiquitination Regulates Chromatin Condensation and Anti-Cancer Drug Response. Cancers. 2022, 14(15): 3732. 4. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay. Talanta. 2016, 161: 804-811. 5. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 6. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684.
Stachyose tetrahydrate Ursonic Acid KRAS inhibitor-9 [8]-Shogaol BAY 11-7082 Tubulin polymerization-IN-43 5-Methoxyuridine TAS6417

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌上市药物库 抗癌药物库 微管靶向化合物库 药物功能重定位化合物库 肝脏毒性化合物库 儿童药物库 自噬库 FDA 上市药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

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