Paclitaxel(Synonyms: 紫杉醇)

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Paclitaxel (Synonyms: 紫杉醇) 纯度: 99.96%

Paclitaxel 是一种天然抗肿瘤药,可稳定微管蛋白 (tubulin) 的聚合。Paclitaxel 可导致有丝分裂停滞和诱导细胞凋亡 (apoptosis),最终导致细胞死亡。Paclitaxel 还可诱导细胞自噬 (autophagy)。

Paclitaxel(Synonyms: 紫杉醇)

Paclitaxel Chemical Structure

CAS No. : 33069-62-4

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10 mM * 1 mL in DMSO ¥572 In-stock
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生物活性

Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].

IC50 & Target[1]

Traditional Cytotoxic Agents

 

体外研究
(In Vitro)

Paclitaxel (20 nM; 48 hours) induces programmed cell death and exists a block at the G2/M phase of the cell cycle[1].
Paclitaxel (20 nM; 48 hours) induces a consistent increase in the level of p53[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: MCF-7, MDA-MB-231 cells
Concentration: 20 nM
Incubation Time: 48 hours
Result: Induced programmed cell death.

Cell Cycle Analysis[1]

Cell Line: MCF-7, MDA-MB-231 cells
Concentration: 20 nM
Incubation Time: 48 hours
Result: >60% of MCF-7 cells and 50% of MDA-MB-231 cells were in the G2/M phase following 24 h treament.

Western Blot Analysis[1]

Cell Line: MCF-7 cells (harboring wild-type p53)
Concentration: 20 nM
Incubation Time: 48 hours
Result: Induced a consistent increase in the level of p53.

体内研究
(In Vivo)

Paclitaxel (1-20 mg/kg; i.p.; 1 time/2 days for five cycles) obviously induces liver metastases at the low-Paclitaxel group with little influence on primary tumor growth[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA-231 xenograft-bearing mice[3]
Dosage: 1, 20 mg/kg
Administration: Intraperitoneal injection; five cycles (1 time/2 days)
Result: Liver metastases were obviously induced in the low-PTX (1 mg/kg) group with little influence on primary tumor growth compared with high-PTX group.

Clinical Trial

分子量

853.91

Formula

C47H51NO14

CAS 号

33069-62-4

中文名称

紫杉醇

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (117.11 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1711 mL 5.8554 mL 11.7108 mL
5 mM 0.2342 mL 1.1711 mL 2.3422 mL
10 mM 0.1171 mL 0.5855 mL 1.1711 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.44 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.44 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.44 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.

    [2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.

    [3]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Aug;283(15):2836-52.

    [4]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.

    [5]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.

    [6]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.

    [7]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.

    [8]. Jing C, et al. E7080 enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.