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Paclitaxel (Taxol)

现货
Catalog No.
A4393
抗肿瘤药
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
50mg
¥ 500.00
现货
100mg
¥ 800.00
现货
500mg
¥ 1,400.00
现货

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Background

Paclitaxel is a novel antineoplastic agent, which was discovered in a screen of extracts of thousands of plants and natural products for antineoplastic activity by a National Cancer Institute program. Alought it functions as a mitotic inhibitor like vinca alkaloids, paclitaxel promotes the polymerization of tubulin instead of inducing the disassembly of microtubules, which inhibits the microtubules disassembly and promotes the formation of excessively stable, dysfunctional microtubules. Paclitaxel has exhibited antitumor activity against a broad spectrum of human cancers, including ovarian, breast, head and neck, and lung cancer, in a large number of studies.

Reference

Ross C. Donehower. The clinical development of paclitaxel: a successful collaboration of academia, industry and the National cancer Institute. STEM CELLS 1996;14:25-28

文献引用

1. Chung HK, Zou X, et al. "A compact synthetic pathway rewires cancer signaling to therapeutic effector release. Science." 2019 May 3;364(6439). PMID:31048459
2. 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
3. Deng Y, Li F, et al. "Triptolide sensitizes breast cancer cells to Doxorubicin through the DNA damage response inhibition." Mol Carcinog. 2018 Jun;57(6):807-814. PMID:29500880
4. Zina Hamoudi , Thang Manh Khuong, et al. "A fruit fly model for studying paclitaxel-induced pain [version 1;referees: awaiting peer review]" F1000Research 23 Jan 2018, 7:99.
5. Yu Wang,Zhenxin Zhu, et al. "The effect of phenotypic conditioned medium on the proliferation of BGC823 in human gastric cancer cell line." Academic Journal of Second Military Medical University,Dec.2017,Vol.38,No.12.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt853.91
Cas No.33069-62-4
FormulaC47H51NO14
SynonymsTaxol
Solubility≥42.6955mg/mL in DMSO, ≥31.6 mg/mL in EtOH with ultrasonic, <4.46 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](OC(C)=O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@H]4C[C@@H]3O)([H])[C@@H]2OC(C5=CC=CC=C5)=O)=O)=C1C)=O)O)C6=CC=CC=C6)C7=CC=CC=C7
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

人类动脉内皮细胞(haEC)

制备方法

该化合物在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℃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℃可放置数月。

反应条件

1 μM,24 hours

实验结果

进行不间断和单剂量(24小时)给药6天后,通过细胞计数、BrdU-ELISA和MTT实验测定细胞增殖。在高浓度(0.01至1.0 μmol/L)下,paclitaxel以剂量依赖性方式显著抑制细胞生长,而较低的紫杉醇剂量(0.1至1.0 nmol/L)对haEC生长的抑制效果不明显。此外,在该浓度范围内没有观察到非特异性细胞毒性作用。

动物实验: [2]

动物模型

雌性CB17 SCID小鼠

给药剂量

静脉注射,12.5 mg/kg

实验结果

在用紫杉醇处理的小鼠中,肿瘤和真皮移植物之间的界面不明确,在人真皮内观察到小组肿瘤细胞,肿瘤细胞被扩张的血管包围。血管横截面的定量证实了组织学效果,与紫杉醇和脂质体处理的小鼠相比,在LP治疗的小鼠中,每个高倍视野的血管数量显著减少。

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] Axel D I, Kunert W, G?ggelmann C, et al. Paclitaxel inhibits arterial smooth muscle cell proliferation and migration in vitro and in vivo using local drug delivery. Circulation, 1997, 96(2): 636-645.

[2] Kunstfeld R, Wickenhauser G, Michaelis U, et al. Paclitaxel encapsulated in cationic liposomes diminishes tumor angiogenesis and melanoma growth in a “humanized” SCID mouse model. Journal of investigative dermatology, 2003, 120(3): 476-482.

生物活性

描述 Paclitaxel是微管聚合物的稳定剂,在人内皮细胞中的IC50值为0.1 pM。
靶点 Microtubule (human endothelial cells)          
IC50 0.1 pM          

质量控制

化学结构

Paclitaxel (Taxol)

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