Paclitaxel (NSC 125973)

Paclitaxel是一种微管聚合物稳定剂，作用于人内皮细胞，IC50为0.1 pM结合β-微管蛋白的N -端区域，促进了高度稳定的微管形成体，抵制解聚，防止正常细胞分裂和捕获在细胞周期的G2 / M期。 Information Paclitaxel (NSC 125973, PTX, Taxol, Onxal, Abraxane) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. In vitro Paclitaxel inhibits non-endothelial type human cells at 10 4 - to 10 5 -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 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. Cell Data cell lines： HT29, SW620 and MDA-MB-231 cells Concentrations： 0.1-100 pM Incubation Time： 72 hours Powder Purity:≥98%

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