| 名称 | Paclitaxel |
| 描述 | Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy. |
| 细胞实验 | 1×10^4 cells are plated in 100 μL of the growth medium in the presence or absence of increasing concentrations (0.1-1 μM) of taxol in 96-well plates and cultured at 37°C in 5% CO2 for 12-48 h. The cells are then incubated with 25 μL of MTT (5 mg/mL) at 37°C for 4 h. After dissolving the crystals with 0.04 N HCl in isopropanol, the plates are read in a microplate reader at 570 nm [1]. |
| 激酶实验 | To determine which caspases are involved in apoptosis induced by taxol, caspase-3 inhibitor (DEVD-CHO), caspase-6 inhibitor (Z-VEID-FMK), caspase-8 inhibitor (Z-IETD-FMK or IETD-CHO), caspase-9 inhibitors (Z-LEHD-FMK or LEHD-CHO), and caspase-10 inhibitor (Z-AEVD-FMK) are used. These caspase inhibitors are dissolved in dimethyl sulfoxide (Me2SO); the final concentration of Me2SO is 0.1%. Cells (5×105) are preincubated in the presence or absence of 100 μM?each of these inhibitors for 3 h at 37°C then treated with or without 0.1, 0.5, and 1 μM?Paclitaxel for 48 h and processed for annexin V binding assay [1]. |
| 动物实验 | Adult (250-320 g) male Sprague-Dawley rats are used for all experiments. One week following the DiI injection, rats are anesthetized with isofluorane and injected into the tail vein with 2 mg/kg paclitaxel or its vehicle (1:1:23, cremophor EL:ethanol:0.9% saline). The tail vein injection is repeated three more times every other day for a total of four injections [4]. |
| 体外活性 | 方法：人 T 细胞淋巴细胞白血病细胞 CCRF-HSB-2 用 Paclitaxel (0.01-1 µM) 处理 48 h，使用 MTT 方法检测细胞生长抑制情况。
结果：Paclitaxel 剂量依赖性地抑制 CCRF-HSB-2 细胞生长，IC50 为 0.25 µM。[1]
方法：人胃癌细胞 AGS 用 Paclitaxel (10-160 nM) 处理 24-48 h，使用 Western Blot 方法检测靶点蛋白表达水平。
结果：Paclitaxel 诱导凋亡相关蛋白 cleaved caspase-3 和 cleaved PARP 表达上调。[2]
方法：犬乳腺肿瘤细胞 CHMm 用 Paclitaxel (0.01-1 μM) 处理 24 h，使用 Flow Cytometry 方法检测细胞凋亡情况。
结果：Paclitaxel 剂量依赖性诱导 CHMm 细胞凋亡。[3] |
| 体内活性 | 方法：为研究低剂量 Paclitaxel 对肿瘤侵袭的影响，将 Paclitaxel (2.6 mg/kg) 腹腔注射给药给携带胆管癌肿瘤 EGI-1 的 SCID 小鼠，每天一次，持续两周。
结果：低剂量 Paclitaxel 治疗减少了 EGI-1 细胞的肺扩散，而不显著影响其局部肿瘤生长。[4]
方法：开发 Paclitaxel 醇诱导的负面情感症状的临床前模型，将 Paclitaxel (2-8 mg/kg in 1 volume ethanol+1 volume Emulphor-620 +18 volumes distilled water) 腹腔注射给 C57BL/6J 小鼠，每两天一次，共注射四次。
结果：8 mg/kg Paclitaxel 处理导致机械性和冷性异常性疼痛的发展和维持。Paclitaxel 也诱导了焦虑样行为和抑郁样行为。Paclitaxel 在小鼠情感状态建模试验中产生了行为改变，而伤害性反应的增加持续时间更长。[5] |
| 存储条件 | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 21.4 mg/mL (25.06 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.54 mg/mL (10 mM), Suspension.
DMSO : 257.5 mg/mL (301.55 mM), Sonication is recommended.
|
| 关键字 | Paclitaxel | NSC-125973 | NSC125973 | MicrotubuleAssociated | Microtubule/Tubulin | Microtubule Associated | microtubule | Inhibitor | inhibit | Autophagy | Apoptosis | ADCCytotoxin | ADC Payload | ADC Cytotoxin |
| 相关产品 | Formamide | Urea | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Tamoxifen | Paeonol |
| 相关库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 植物来源化合物库 | EMA 上市药物库 | 药食同源库 | 抗衰老化合物库 | 天然产物库 | 药物功能重定位化合物库 | 微管靶向化合物库 | 抗癌临床化合物库 | 抗癌药物库 |