Paclitaxel

製品コードS1150 バッチS115015

化学情報

	Synonyms	NSC 125973，PTX	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₄₇H₅₁NO₁₄
	分子量	853.91	CAS No.	33069-62-4
Solubility (25°C)*	体外	DMSO	100 mg/mL (117.1 mM)
		Ethanol	25 mg/mL (29.27 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	パクリタキセル (Paclitaxel (NSC 125973, PTX)) は微小管を安定化することで脱重合を阻害します。ヒト血管内皮細胞における IC50 は 0.1 pM です。
in vitro	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. ^[1] 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. ^[2] Paclitaxel alone causes a time-dependent inhibition of CDK1 in four cell lines including A549 cells, H358, H1395 cells and H1666 cells. ^[3]
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. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cells including human neonatal dermal microvascular ECs (HMVECs), human umbilical vein ECs (HUVECs), human umbilical artery ECs (HUAVECs), normal human astrocytes (NHAs), normal human dermal fibroblasts (NHDFs), normal human epidermal keratinocytes (NHEKs
	濃度	0.1-100 pM
	反応時間	72 hours
	実験の流れ	Cells including human neonatal dermal microvascular ECs (HMVECs), human umbilical vein ECs (HUVECs), human umbilical artery ECs (HUAVECs), normal human astrocytes (NHAs), normal human dermal fibroblasts (NHDFs), normal human epidermal keratinocytes (NHEKs), human mammary epithelial cells (HMEpCs), human prostate epithelial cells (PrEpCs) and human umbilical artery smooth muscle cells (UASMCs) are cultured. Cell proliferations are performed in 96-well plates using cells between passages 6 and 12. Cells are seeded at 3000–5000 cells/well and allowed to attach for 4 hours. Paclitaxel, diluted in culture medium, is added in quadruplicate wells and the cells ae incubated for 3 days before MTS reagents are added to quantitate the live cells in each well.
動物実験	動物モデル	Female, 20-22 g homozygous nude athymic mice with BC-V and BC-ER tumors
	投薬量	20 mg/kg
	投与方法	Administered via i.v.

参考

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カスタマーフィードバック

: Data from [RSC Adv, 2011, 1, 884-892]

: Data from [Data independently produced by , , Science, 2018, 10(433), doi: 10.1126/scitranslmed.aar1916]

: Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(15):4364-4375]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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