| 名稱 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 體外活性 | 每4天注射3次33 mg/kg Docetaxel導(dǎo)致M2OL2結(jié)腸癌異種移植瘤的生長(zhǎng)延遲19.3天.在MX-1,SK-MEL-2,LX-1和OVCAR-3 異種移植物中,Docetaxel具有良好的抗腫瘤活性.一周注射兩次Docetaxel,持續(xù)14天,抑制成纖維細(xì)胞生長(zhǎng)因子2的血管生成反應(yīng),IC 50為5.4 mg/kg.當(dāng)給藥10 mg/kg Docetaxel時(shí),會(huì)完全抑制小鼠的血管生成. |
| 體內(nèi)活性 | Docetaxel抑制人癌細(xì)胞Hs746T (胃),AGS (胃),HeLa (子宮頸),CaSki (子宮頸),BxPC3 (胰腺),Capan-1 (胰腺)的克隆存活,IC50 分別為1 nM,1 nM,0.3 nM,0.3 nM,0.3 nM 和 0.3 nM。DDocetaxel可以抑制兩個(gè)血管生成因子,胸苷磷酸化酶或VEGF刺激的人臍靜脈血管內(nèi)皮細(xì)胞趨藥性,IC50 為10 pM。Docetaxel誘導(dǎo)人單核細(xì)胞,而不影響RAW 264.7 小鼠巨噬細(xì)胞中前列腺素H 合酶-2m (PGHS-2)的表達(dá)。 |
| 存儲(chǔ)條件 | 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.
10% DMSO+90% Saline : < 10 mg/mL (11.6 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 250 mg/mL (290.04 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (11.6 mM), Solution.
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| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 抗癌活性化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 臨床失敗化合物庫(kù) | EMA 上市藥物庫(kù) | 抗衰老化合物庫(kù) | FDA 上市藥物庫(kù) | 微管靶向化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) |