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)。
| 生物活性 | Paclitaxel is a naturally occurring antineoplastic agent and stabilizestubulinpolymerization. Paclitaxel can cause both mitotic arrest andapoptoticcell death. Paclitaxel also inducesautophagy[1][2]. |
| IC50& Target[1] | Traditional Cytotoxic Agents |
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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].
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. |
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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].
| 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. |
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| 来源 | - Plants
- Taxaceae
- Taxus chinensis(Pilger) Rehd.
- Plants
- Illiciaceae
- Taxus chinensis(Pilger) Rehd.
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： corn oil Solubility: 10 mg/mL (11.71 mM); Suspended solution; Need ultrasonic 2. 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 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本网站选购。
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