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Docetaxel

现货
Catalog No.
A4394
微管解聚抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 700.00
现货
50mg
¥ 500.00
现货
100mg
¥ 600.00
现货

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Background

Docetaxel, a new taxoid family member originally derived from the needles of the European Yew tree Taxus baccata, is a potent chemotherapeutic agent that acts as a spindle poison to inhibit microtubule dynamics and cell cycle arrest through promoting microtublin assembly and stabilizing the polymers against depolymerization. Docetaxel has demonstrated strong in vivo and in vitro antitumor activities against a broad range of cancers including breast, lung, ovarian, head and neck, and gastric cancers. Previous studies have shown that docetaxel exertss stronger cytotoxicity than other chemotherapeutic agents against ovarian carcinoma cell lines, in which the cytotoxicity of docetaxel is 1.2-2.6 times greater than that of paclitaxel and over 1000 times greater than that of cisplatin or etoposide.

Reference

N Katsumata. Docetaxel: an alternative taxane in ovarian cancer. British Journal of Cancer (2003) 89 (Suppl 3), S9-S15

文献引用

1. Zhang Y, Xia F, et al. "miR-135b-5p enhances doxorubicin-sensitivity of breast cancer cells through targeting anterior gradient 2." J Exp Clin Cancer Res. 2019 Jan 21;38(1):26. PMID:30665445
2. Li Q, Deng Q, et al. "Linking prostate cancer cell AR heterogeneity to distinct castration and enzalutamide responses." Nat Commun. 2018 Sep 6;9(1):3600. PMID:30190514
3. Zhou XW, Xia YZ, et al. "Tomentodione M sensitizes multidrug resistant cancer cells by decreasing P-glycoprotein via inhibition of p38 MAPK signaling. Oncotarget." 2017 Oct 19;8(60):101965-101983. PMID:29254218

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt807.88
Cas No.114977-28-5
FormulaC43H53NO14
SynonymsTaxotere, Docetaxel anhydrous, Trihydrate
Solubility≥40.4mg/mL in DMSO, ≥94.4 mg/mL in EtOH, <2.17 mg/mL in H2O
SDFDownload SDF
Canonical SMILESO=C(N[C@H]([C@H](C(O[C@H]1C[C@]2(O)C(C)(C)C([C@@H](O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@@]4([H])C[C@@H]3O)([H])[C@@H]2OC(C5=CC=CC=C5)=O)=O)=C1C)=O)O)C6=CC=CC=C6)OC(C)(C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

9种人胃癌细胞系

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

< 0.00012 ~ > 1.2 μM

实验结果

在9种人胃癌细胞系中,Docetaxel对其中6种细胞显示出较强的细胞毒性(相对于Paclitaxel)。相对于其它7种细胞系,Docetaxel和Paclitaxel对MM-7和ST-SA-1细胞的影响相对较少。

动物实验 [1]:

动物模型

携带人胃癌异种移植瘤(MKN-28、MKN-45和KKLS)的小鼠模型

给药剂量

3.75、7.5、15或22 mg/kg;静脉注射;每4天注射3次

实验结果

Docetaxel呈剂量依赖性抑制肿瘤生长。对于所有小鼠,在剂量为15和22 mg/kg时,Docetaxel诱导肿瘤完全消退。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Tanaka M, Obata T, Sasaki T. Evaluation of antitumour effects of docetaxel (Taxotere) on human gastric cancers in vitro and in vivo. Eur J Cancer. 1996 Feb;32A(2):226-30.

生物活性

描述 Docetaxel是一种紫杉醇的类似物,通过结合到稳定的微管抑制微管解聚。
靶点 Microtubules          
IC50            

质量控制

化学结构

Docetaxel

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