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Docetaxel trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂,抑制微管解聚的IC50值为 0.2 μM。它是紫杉醇的半合成类似物,能减弱 bcl-2 和 bcl-xL 基因表达的影响。它阻滞G2/M 细胞周期,导致细胞凋亡。
Docetaxel trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂,抑制微管解聚的IC50值为 0.2 μM。它是紫杉醇的半合成类似物,能减弱 bcl-2 和 bcl-xL 基因表达的影响。它阻滞G2/M 细胞周期,导致细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 327 | 现货 | |
100 mg | ¥ 460 | 现货 | |
500 mg | ¥ 1,110 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 240 | 现货 |
产品描述 | 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. |
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。 |
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) |
别名 | 多西他赛三水合物, RP-56976 (Trihydrate), RP56976 (NSC 628503) Trihydrate |
分子量 | 861.95 |
分子式 | C43H59NO17 |
CAS No. | 148408-66-6 |
Smiles | O.O.O.CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@]1(C)[C@@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)C(O)C(NC(=O)OC(C)(C)C)c3ccccc3)C(C)=C([C@@H](O)C1=O)C2(C)C |
密度 | 1.37 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 100 mg/mL (116.01 mM) DMSO: 100 mg/mL (116.01 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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