Paclitaxel

PaclitaxelCAS号: 33069-62-4分子式: C47H51NO14分子量: 853.91描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述

Paclitaxel (紫杉醇) 是微管聚合稳定剂,IC50是0.1 pM。Paclitaxel 是有丝分裂抑制剂。

纯度
>99 %
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
紫杉醇;NSC 125973;Taxol
外观
Lyophilized powder
可溶性/溶解性
DMSO:171 mg/mL (200.25 mM)

Ethanol:18 mg/mL (21.07 mM)

生物活性
靶点
Microtubule (human endothelial cells)
In vitro(体外研究)
Paclitaxel inhibits non-endothelial type human cells at 104 – to 105 -fold higher concentrations, with IC50 of 1 nM-10 nM. The selectivity of Paclitaxel inhibition of cell proliferation is also species specific, as mouse ECs are not sensitive to Paclitaxel at ultra low concentrations. Inhibition of human ECs by Paclitaxel at ultra low concentrations does not affect the cellular microtubule structure, and the treated cells do not show G2/M cell cycle arrest and apoptosis, suggesting a novel but as yet unidentified mechanism of action. In an in vitro angiogenesis assay, Paclitaxel at ultra low concentrations blocks human ECs from forming sprouts and tubes in the three-dimensional fibrin matrix. In the presence of SMF, the efficient concentration of Paclitaxel on K562 cells is decreased from 50 to 10 ng/mL. The cell cycle arrest effect of Paclitaxel with or without SMF on K562 cells is correlated with DNA damage. Paclitaxel alone causes a time-dependent inhibition of CDK1 in four cell lines including A549 cells, H358, H1395 cells and H1666 cells.
In vivo(体内研究)
The inhibition rations of Paclitaxel alone on BC-V and BC-ER tumors are 49.78% and 51.23%, respectively. Treatment of six cycles of 20 mg/kg Paclitaxel significantly reduces the percentages of Ki-67-positive cells to 20.4% in BC-V tumors and 25.1% in BC-ER tumors, respectively.
参考文献
参考文献
[1] Wang J, et al. Anticancer Drugs. 2003, 14(1), 13-19.
[2] Sun RG, et al. Gen Physiol Biophys. 2012, 31(1), 1-10.
[3] Zhang XH, et al. Cancer Lett. 2012, 322(2), 213-222.
[4] Chang J, et al. Breast Cancer Res Treat. 2012.

分子结构图

Paclitaxel