紫杉醇(Paclitaxel,Taxol),CAS NO.33069-62-4,一种抗肿瘤化合物和微管聚合物稳定剂

Cisplatin顺铂;Oxaliplatin奥沙利铂;DNA Crosslinker DNA交联剂;Cyclophosphamide环磷酰胺;CAS:33069-62-4;

产品描述

紫杉醇(Paclitaxel,Taxol),CAS NO.33069-62-4,一种抗肿瘤化合物和微管聚合物稳定剂。对一组肿瘤细胞包括宫颈癌(HeLa),肺癌(A549),乳腺癌(MCF-7),结肠癌(HT-29),卵巢癌(OVG-1)和胰脏癌(PC-Sh)细胞进行紫杉醇的细胞毒性测试,IC50s= 2.5-7.5 nM。各种癌细胞系中,紫杉醇破坏多极纺锤体形成,诱导细胞周期停滞在前期和G1期,IC50s= 6.7-18.5 nM。紫杉醇启动癌细胞凋亡,通过p53依赖和非依赖途径,Bcl-2家族蛋白,细胞周期蛋白依赖的激酶和JNK/SAPK参与的多种机制来发挥作用。紫杉醇是神经突起生长和启动的一种抑制剂,通过破坏生长中突起的微管组装和移除细胞质的微管来发挥作用。紫杉醇是PKA和Raf-1的强效激活剂。

产品特性

1) CAS NO:33069-62-4

2) 化学名:βS-(benzoylamino)-αR-hydroxy-benzenepropanoic acid, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS) -6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester

3) 同义名:Taxol,NSC 125973

4) 分子式:C47H51NO14

5) 分子量:853.92

6) 纯度:≥99%

7) 外观:白色或类白色结晶性粉末

8) 溶解性:溶于DMSO(80mg/ml)、乙醇(10mg/ml),几乎不溶于水

保存与运输方法

保存:2-8℃干燥保存,也可置于-20ºC干燥长期保存,至少2年有效。

运输:室温运输。

使用方法【源自文献,仅作参考】

文献1,Elzbieta Izbicka et al.Biomarkers for Sensitivity to Docetaxel and Paclitaxel in Human Tumor Cell Lines In Vitro.CANCER GENOMICS & PROTEOMICS 2: 219-226 (2005).

体外研究(细胞实验):

细胞类型(Cell type):LNCaP prostate, SK-MES,MCF-7 and MDA-MB-231,MV-522 lung carcinoma cell lines

药物浓度(Concentration):1000 pM for all cell lines in 3- and 5-day exposures, with the exception for500 pM paclitaxelin MDA-MB-231 for a 5-day treatment.A 10 mM stock solution of paclitaxel was prepared in 100% DMSO, and all dilutions contained 0.1% DMSO.

文献2,Park SJ et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3; 279(49): 51057-67.PMID: 15452117

体外研究(细胞实验):

细胞类型(Cell type):CCRF-HSB-2 human T-cell lymphoblastic leukemia cell line

药物浓度(Concentration):For MTT assay, 1 × 104 cells were plated in 100 μl of the growth medium in the presence or absence of increasing concentrations (0.1–1 μM) of taxolin 96-well plates and cultured at 37 °C in 5% CO2 for 12–48 h. The results revealed thattaxol at 0.1, 0.5, and 1 μM reduced the proliferation and survival of CCRF-HSB-2 cells in a dose-dependent fashion and that the IC50 value of taxol was about 0.25 μM.

文献3,Huehnchen P et al.Assessment of Paclitaxel Induced Sensory Polyneuropathy with “Catwalk” Automated Gait Analysis in Mice.PLoS One. 2013 Oct 15;8(10): e76772. PMID: 24143194

体内研究(动物模型):

动物模型(Animal Model):85 nine-week old male C57BL/6J mice

注射剂量(Dosages):20 mg PTX/kg BW,dissolved in Cremophor EL: Ethanol (1:1) with a concentration of 6 mg/ml and diluted in sterile 0.9% NaCl solution to a final concentration of 2 mg/ml before injection

给药途径(Administration):Intraperitoneal (i.p.) injection

文献4,Cadamuro M et al. Low-Dose Paclitaxel Reduces S100A4 Nuclear Import to Inhibit Invasion and Hematogenous Metastasis of Cholangiocarcinoma. Cancer Res. 2016 Aug 15;76(16):4775-84. PMID: 27328733

体内研究(动物模型):

动物模型(Animal Model):SCID mice xenotransplanted with human EGI-1 cells

注射剂量(Dosages):Once tumor engraftment was confirmed by bioluminescence imaging (time 0), we started metronomic infusion ofpaclitaxel [diluted in a 50%/50% solution of Cremophor EL and ethanol (vehicle)] for 2 weeks at the dosage of 2.6 mg/kg/day by intraperitoneal injection using micro-osmotic pumps.

注意事项

1) 本品水溶性非常差,可使用聚氧乙烯蓖麻油(Cremophor EL)和无水乙醇(1:1)用作增溶剂。

2) 本品用于体内动物实验,可使用溶剂5% DMSO+5% Tween 80+ddH2O依此加入来溶解粉末,浓度约2.5mg/ml;或者参考文献结合给药方式,选择其他适当溶剂体系。

3) 本品不是临床药物,只能用于科研用途,不能用于诊断或临床用途。

4) 为了您的安全和健康,请穿实验服并戴一次性手套操作。

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