Docetaxel 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 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.

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.

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。

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)

148408-66-6

C43H59NO17

861.935

RP56976 (NSC 628503) Trihydrate;多西他赛三水合物;RP-56976 (Trihydrate)

H2O:<1 mgml
Ethanol:100 mg/mL (116.01 mM)
DMSO:100 mg/mL (116.01 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years