多西他赛|T1034

Docetaxel
114977-28-5

￥198 10瓶起订

￥153 5瓶起订

￥958 200瓶起订

￥1580 500瓶起订

￥453 50瓶起订

￥656 100瓶起订

￥318 25瓶起订

￥597 1瓶起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 多西他赛

英文名称：: Docetaxel

CAS号：: 114977-28-5

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.29%

产品类别：: 抑制剂

货号：: T1034

Product Introduction

Bioactivity

名称	Docetaxel
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.
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].
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]
存储条件	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 80.8 mg/mL (100 mM) DMSO : 60 mg/mL (74.27 mM)
关键字	Docetaxel \| NSC628503 \| Endogenous Metabolite \| inhibit \| Inhibitor \| Apoptosis \| RP 56976 \| RP56976 \| NSC-628503 \| Microtubule/Tubulin
相关产品	Formamide \| Guanidine hydrochloride \| Naringin \| Daidzein \| Glycerol \| Sucrose \| Ferulic Acid \| Stavudine \| Thymidine \| Fumaric acid
相关库	抗癌上市药物库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA 上市药物库 \| 微管靶向化合物库 \| 药物功能重定位化合物库 \| 萜类天然产物库 \| 抗癌临床化合物库

NSC 628503|||RP-56976|||多西他赛|||多烯紫杉醇

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子