产品说明书

Paclitaxel

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Chemical Structure| 33069-62-4 同义名 : NSC 125973;NSC 125973,PTX
CAS号 : 33069-62-4
货号 : A238238
分子式 : C47H51NO14
纯度 : 99%
分子量 : 853.906
MDL号 : MFCD00869953
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(122.96 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

动物实验配方:

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 40 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]. Paclitaxel can stabilize the microtubule formation through interacting with β-tubulin[2] and then promoting the polymerization and assembly of it[3]. Paclitaxel show the inhibitory effect on HMVEC proliferation with IC50 of 0.1 pM, much lower than the IC50 of 5-FU, camptothecin, cisplatin and doxorubicin[4]. Paclitaxel induces G2/M arrest of cell cycle, thus it also used in synchronization in cell cycle[5]. Paclitaxel was approved by FDA in treatment of ovarian cancer, breast cancer, non-small-cell lung cancer[6], etc..
作用机制 Paclitaxel can stabilize the microtubule formation through interacting with β-tubulin[2] and then promoting the polymerization and assembly of it[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=0.0015 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.00796 μM SANGER
A101D Growth Inhibition Assay IC50=0.0096 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.17mL

0.23mL

0.12mL

5.86mL

1.17mL

0.59mL

11.71mL

2.34mL

1.17mL

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]Snyder JP, Nettles JH, et al. The binding conformation of Taxol in beta-tubulin: a model based on electron crystallographic density. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5312-6. Epub 2001 Apr 17.

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

[4]Wang J, Lou P, et al. Paclitaxel at ultra low concentrations inhibits angiogenesis without affecting cellular microtubule assembly. Anticancer Drugs. 2003 Jan;14(1):13-9.

[5]Trielli MO, Andreassen PR, et al. Differential Taxol-dependent arrest of transformed and nontransformed cells in the G1 phase of the cell cycle, and specific-related mortality of transformed cells. J Cell Biol. 1996 Nov;135(3):689-700.

[6]Shi X, Sun X, et al. Regulation of paclitaxel activity by microtubule-associated proteins in cancer chemotherapy. Cancer Chemother Pharmacol. 2017 Nov;80(5):909-917.

[7]Sparreboom A, van Tellingen O, et al. Nonlinear pharmacokinetics of paclitaxel in mice results from the pharmaceutical vehicle Cremophor EL. Cancer Res. 1996 May 1;56(9):2112-5.

[8]Cividalli A, Cruciani G, et al. Greater antitumor efficacy of paclitaxel administered before epirubicin in a mouse mammary carcinoma. J Cancer Res Clin Oncol. 1998;124(5):236-44.

[9]Jin J, Cai D, et al. Comparative pharmacokinetics of paclitaxel after oral administration of Taxus yunnanensis extract and pure paclitaxel to rats. Fitoterapia. 2013 Oct;90:1-9.