Paclitaxel

パクリタキセル(タキソール、Onxol、Nov-Onxol)は、人間の内皮細胞の0.1pMのIC50による微小管ポリマー安定剤です。

目録号S1150
4.5 5 1レビュー 7製品表彰状
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Paclitaxel 化学構造
分子量: 853.91

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Quality Control & MSDS

製品情報

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  • 研究分野

製品の説明

生物活性

情報 パクリタキセル(タキソール、Onxol、Nov-Onxol)は、人間の内皮細胞の0.1pMのIC50による微小管ポリマー安定剤です。
目標 Microtubule (human endothelial cells)
IC50 0.1 pM [1]
In vitro試験 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試験 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]
臨床試験 Paclitaxel has entered in a Phase III clinical trial for the treatment of tubular breast cancer stage II, mucinous breast cancer stage II, breast cancer female NOS and invasive ductal breast cancer.
特集

推薦された実験操作 (公開の文献だけ)

細胞アッセイ: [1]

細胞系 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
処理時間 72 hours
方法 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: [4]

動物モデル Female, 20-22 g homozygous nude athymic mice with BC-V and BC-ER tumors
製剤 Control
投薬量 20 mg/kg
管理 Administered via i.v.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Paclitaxel SDF
分子量 853.91
化学式

C47H51NO14

CAS No. 33069-62-4
保管 2年-20℃
6月-80℃in DMSO
別名 NSC 125973
溶解度 (25°C) * In vitro DMSO 171 mg/mL (200 mM)
<1 mg/mL (<1 mM)
エタノール 18 mg/mL (21 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
* <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.
化学名 Benzenepropanoic acid, β-(benzoylamino)-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-

研究分野

カスタマーレビュー (1)


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Rating
Source RSC Adv , 2011, 1, 884-892. Paclitaxel purchased from Selleck
Method Microscope image
Cell Lines U937 cells
Concentrations
Incubation Time 24 h
Results The ODS-treated cells in Fig. b looked identical to the untreated cells in Fig. a with a similar rate of natural cell death of less than 3%. When Taxol microcrystals are added to the cell culture (the standard way that Taxol is released into biological systems), decreased cell proliferation rate, pronounced swelling and vacuolization are observed, as shown in Fig. c.

製品表彰状 (7)

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