多西他赛 T1034

Product Introduction
Bioactivity


英文名: Docetaxel

描述: 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。

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 sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

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: Abacavir | BS-181 | β-Elemene | Importazole | STAT5-IN-2 | PIK-75 hydrochloride | Neogambogic acid | Urolithin A | 3-Methoxy-9H-Carbazole | Anticancer agent 133

相关库: Drug Repurposing Compound Library | Microtubule-Targeted Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Natural Product Library for HTS | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途