产品说明书

Docetaxel

Print
Chemical Structure| 114977-28-5 同义名 : 多西他赛;多烯紫杉醇 ;RP-56976
CAS号 : 114977-28-5
货号 : A180270
分子式 : C43H53NO14
纯度 : 98+%
分子量 : 807.879
MDL号 : MFCD00800737
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(129.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(61.89 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 7 mg/mL clear

PO 0.5% CMC-Na 37 mg/mL suspension

生物活性
描述 Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor[1]. Docetaxel, belong to the taxane family including paclitaxel, can promote the assembly and polymerization of microtubule[2] with an appearance of twice as active in depolymerization inhibition compared with paclitaxel[3]. When treated with Docetaxel for 72h, the significant growth inhibition can be observed in ovarian cancer cell line, including A2780, H134, IGROV-1 and OVCAR-3, with IC50 ranging from 2.8 - 87 nM. Activation of caspase, upregulation of Bcl-2 phosphorylation and apoptosis can be observed in cells with prolonged G2/M arrest by Docetaxel, which may be one of the mechanism for cell death induced by Docetaxel in tumor therapy[4]. However, Docetaxel also shows antiangiogenic effect in in vitro and in vivo studies. It can inhibit HUVEC proliferation in a dose-dependent manner with an IC50 of 0.27 ng/ml, as well as reduce 54% of angiogenesis level compared with control on dose of 3 mg/kg in MCF-7 tumor bearing nude mice[5]. Docetaxel is approved by FDA for treatment of head and neck cancer, gastric cancer, breast cancer, prostate cancer and non-small cell lung cancer (see in FDA net).
作用机制 Docetaxel can promote the assembly and polymerization of microtubule[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
22RV1 Growth Inhibition Assay IC50=0.00315 μM SANGER
23132-87 Growth Inhibition Assay IC50=0.00155 μM SANGER
5637 Growth Inhibition Assay IC50=0.000143 μM SANGER
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01561456 Non-small-cell Lung Cancer ... 展开 >> Squamous Cell Carcinoma Adenocarcinoma of the Lung 收起 << Phase 2 Completed - Belarus ... 展开 >> State Medical Institution: Republic Scientific Oncology Center Poselok, Minsk Region, Belarus, 223040 Gomel Regional Clinical Oncology Center Gomel, Belarus, 246012 Minsk City Clinical Oncology Center Minsk, Belarus, 220013 Vitebsk Regional Clinical Oncology Center Vitebsk, Belarus, 210603 Hungary Semmelweis University; Clinic for Pulmonology Budapest, Hungary, 1125 University of Debrecen Medical and Health Science Center, Clinic of Pulmonology Debrecen, Hungary, 4042 Kenezy Gyula County Hospital Debrecen, Hungary, 4043 Hospital for Thoracic Diseases of Csongrad County Local Government Deszk, Hungary, 6772 Poland Wladyslaw Bieganski Regional Specialist Hospital Grudziadz, Poland, 86-300 Maria Sklodowska-Curie Institute of Oncology in Warsaw Warsaw, Poland, 02781 Russian Federation State Therapeutical and Prophylactic Institution: Chelyabinsk Regional Oncology Center Chelyabinsk, Russian Federation, 454087 Sverdlovsk Regional Oncology Center Ekaterinburg, Russian Federation, 620036 City Clinical Hospital #1 Novosibirsk, Russian Federation, 630047 Orel Oncology Center Orel, Russian Federation, 302020 State Higher Educational Institution St. Petersburg State Medical University n. a. after I. P. Pavlov under Federal Agency for Healthcare and Social Development, Research Institute of Pulmonology Saint Petersburg, Russian Federation, 197089 St. Petersburg State Medical Institution Municipal Clinical Oncology Center St. Petersburg, Russian Federation, 197022 Tula Regional Oncology Center Tula, Russian Federation, 300053 Ukraine Dnipropetrovsk City Multispecialty Clinical Hospital #4 Dniepropetrovsk, Ukraine, 49102 Public Clinical Treatment and Prophylaxis Institution: Donetsk Regional Antitumor Center Donetsk, Ukraine, 83092 Kharkiv, State Institution: S.P. Hryhoriev Institute of Medical Radiology under the Ukrainian Academy of Medical Sciences Kharkiv, Ukraine, 61024 Public Healthcare Institution: Kharkiv Regional Clinical Oncology Center Kharkiv, Ukraine, 61070 Kyiv City Oncology Hospital Kyiv, Ukraine, 03115 Lviv State Regional Treatment and Diagnostics Oncology Center Lviv, Ukraine, 79031 Zakarpattia Regional Clinical Oncology Center Uzhhorod, Ukraine, 88014 收起 <<
NCT00294385 Breast Cancer Phase 3 Completed - Austria ... 展开 >> 2. Med. Abteilung - LKH-Steyr Steyr, Austria, 4400 Hanusch KrankenhausHämatologisch-Onkologisches Zentrum Vienna, Austria, 1140 Intere IV Krankenhaus Wels Wels, Austria, 4600 Bulgaria Cancer Center Plovdiv Plovdiv, Bulgaria, 4000 SBALO National Oncology Center Sofia, Bulgaria, 1527 SBALO National Oncology Center Sofia, Bulgaria, 1756 Czech Republic FN U sv. Anny Brno, Czech Republic, 656 91 Nemocnice Ceske Budejovice Ceske, Czech Republic FN Hradec Kralove Hradec Kralove, Czech Republic, 500 02 FN Bulovka Prague, Czech Republic, 186 00 Charles University Prague, Dep of Oncology Prague, Czech Republic Israel Rambam Medical Center, Oncol. Dep Haifa, Israel, 31096 Tel Aviv Sourasky Medical Center, Div of Oncology Tel Aviv, Israel "Sheba" Medical Center, Dep of Oncology Tel Hashomer, Israel Lebanon American University of Beirut, Medical Center Beirut, Lebanon Rizk Hospital Beirut, Lebanon Poland Klinika Onkologii CMuJ Krakow, Poland Slovakia Nomocnica Sv. Alzbety, Narodny Onkologicky Ustav Bratislava, Slovakia 收起 <<
NCT00287885 Cervical Cancer ... 展开 >> Endometrial Cancer Fallopian Tube Cancer Ovarian Cancer Peritoneal Cavity Cancer Sarcoma Vaginal Cancer Vulvar Cancer 收起 << Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.24mL

0.25mL

0.12mL

6.19mL

1.24mL

0.62mL

12.38mL

2.48mL

1.24mL
参考文献

[1]Fong KW, Leung JW, et al. MTR120/KIAA1383, a novel microtubule-associated protein, promotes microtubule stability and ensures cytokinesis. J Cell Sci. 2013 Feb 1;126(Pt 3):825-37.

[2]Schiff PB, Fant J, et al. Promotion of microtubule assembly in vitro by taxol. Nature. 1979 Feb 22;277(5698):665-7.

[3]Verweij J, Clavel M, et al. Paclitaxel (Taxol) and docetaxel (Taxotere): not simply two of a kind. Ann Oncol. 1994 Jul;5(6):495-505.

[4]Kolfschoten GM, Hulscher TM, et al. Variation in the kinetics of caspase-3 activation, Bcl-2 phosphorylation and apoptotic morphology in unselected human ovarian cancer cell lines as a response to docetaxel. Biochem Pharmacol. 2002 Feb 15;63(4):733-43.

[5]Sweeney CJ, Miller KD, et al. The antiangiogenic property of docetaxel is synergistic with a recombinant humanized monoclonal antibody against vascular endothelial growth factor or 2-methoxyestradiol but antagonized by endothelial growth factors. Cancer Res. 2001 Apr 15;61(8):3369-72.

[6]van Soest RJ, de Morrée ES, et al. Targeting the Androgen Receptor Confers In Vivo Cross-resistance Between Enzalutamide and Docetaxel, But Not Cabazitaxel, in Castration-resistant Prostate Cancer. Eur Urol. 2015 Jun;67(6):981-985.

[7]202356Orig1s000PharmR