| 名称 | Docetaxel trihydrate |
| 描述 | Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis. |
| 细胞实验 | 2000 cells in 180 μL of medium are seeded in a 96-well plate, and 20 μL of drug solution is simultaneously added in triplicate to each well. The plate is incubated for 3 days at 37°C in a humidified atmosphere of 5% CO2. On day 3, 25 μL of MTT reagent is added to each well. After 4 h of incubation, the medium is removed by aspiration. 0.2 mL of dimethylsulphoxide (DMSO) is added to each well and thoroughly mixed by using a mechanical plate mixer to dissolve the resulting MTT-formazan crystals. Absorbance at 540 nm (OD) is measured by a reader. (Only for Reference) |
| 体外活性 | 每4天注射3次33 mg/kg Docetaxel导致M2OL2结肠癌异种移植瘤的生长延迟19.3天.在MX-1,SK-MEL-2,LX-1和OVCAR-3 异种移植物中,Docetaxel具有良好的抗肿瘤活性.一周注射两次Docetaxel,持续14天,抑制成纤维细胞生长因子2的血管生成反应,IC 50为5.4 mg/kg.当给药10 mg/kg Docetaxel时,会完全抑制小鼠的血管生成. |
| 体内活性 | Docetaxel抑制人癌细胞Hs746T (胃),AGS (胃),HeLa (子宫颈),CaSki (子宫颈),BxPC3 (胰腺),Capan-1 (胰腺)的克隆存活,IC50 分别为1 nM,1 nM,0.3 nM,0.3 nM,0.3 nM 和 0.3 nM。DDocetaxel可以抑制两个血管生成因子,胸苷磷酸化酶或VEGF刺激的人脐静脉血管内皮细胞趋药性,IC50 为10 pM。Docetaxel诱导人单核细胞,而不影响RAW 264.7 小鼠巨噬细胞中前列腺素H 合酶-2m (PGHS-2)的表达。 |
| 存储条件 | 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 : 100 mg/mL (116.02 mM), Sonication is recommended.
DMSO : 100 mg/mL (116.02 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (4.64 mM), Sonication is recommended.
|
| 关键字 | Tubulin β-1 chain | RP56976 (NSC 628503) | RP-56976 | RP56976 | RP 56976 | MicrotubuleAssociated | Microtubule/Tubulin | Microtubule Associated | Inhibitor | inhibit | Docetaxel trihydrate | Docetaxel | Bcl-2 | Apoptosis |
| 相关产品 | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Dextran sulfate sodium salt (MW 5000) | Citric Acid Triammonium | Gum arabic | Stavudine | Tamoxifen | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 抗癌上市药物库 | 抗癌活性化合物库 | 已知活性化合物库 | 生物碱类天然产物库 | EMA 上市药物库 | 抗癌天然产物库 | 抗衰老化合物库 | FDA 上市药物库 | 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 |