Paclitaxel (Taxol)
(Synonyms: 紫杉醇) 目录号 : GC12511
紫杉醇是从短叶红豆杉的树皮和针叶中提取出来的三环二萜化合物。
Cas No.:33069-62-4
Sample solution is provided at 25 µL, 10mM.
Paclitaxel, from the bark and needles of Taxus brevifolia, is a tricyclic diterpenoid compound. Paclitaxel can promote the assembly of tubulin into microtubules and prevent the dissociation of microtubules, blocking cell cycle progression, preventing mitosis, and inhibiting the growth of cancer cells.[1]
In vitro, paclitaxel significantly inhibited the proliferation of ATC cells in a dose-dependent manner; the IC50 value ranged from 1.99 to 9.97 nM.[6] Encapsulating paclitaxel into nano-drug carriers, the water-solubility, selective delivery to cancers, tissue toxicity, controlled release and pharmacokinetic property of paclitaxel are improved, can improve its toxicity to human, keep or enhance its activity and improve its pharmacokinetic property.[2] In vitro, in a short time, exposures to paclitaxel induced the phosphorylation and degradation of IkappaB-alpha, which in turn caused the activation of NF-kappaB in both human breast cancer BCap37 and human epidermoid carcinoma KB cells. [3] In addition, Paclitaxel can increase its cytotoxic effect by the loading of Paclitaxel to autologous prostate cancer cell-derived EVs.[5]
In vivo experiment it shown that treatment with 1 mg/kg and 20 mg/kg paclitaxel, the light-colored spotted metastases were dramatically increased in livers from the low-dose paclitaxel-treated mice and the metastasis was substantially reduced in the high-dose paclitaxel group.[4] In vivo, the growth of C643 cell-derived xenograft tumors in the lenvatinib-treated (5 mg/kg; p.o.) and paclitaxel-treated (5 mg/kg;i.p.) groups was slower than that in control group.[6]
References:
[1]Zhu L, Chen L. Progress in research on paclitaxel and tumor immunotherapy. Cell Mol Biol Lett. 2019 Jun 13;24:40.
[2]Chen S, et al. Recent Development of Copolymeric Nano-Drug Delivery System for Paclitaxel. Anticancer Agents Med Chem. 2020;20(18):2169-2189.?
[3]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.?
[4]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.
[5]Saari H, et al. Microvesicle- and exosome-mediated drug delivery enhances the cytotoxicity of Paclitaxel in autologous prostate cancer cells. J Control Release. 2015 Dec 28;220(Pt B):727-37.?
[6]Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
紫杉醇是从短叶红豆杉的树皮和针叶中提取出来的三环二萜化合物。它可以促进微管蛋白聚集成微管，并防止微管解离，从而阻碍细胞周期进展、预防有丝分裂并抑制癌细胞生长。[1]
在体外实验中，紫杉醇以剂量依赖的方式显著抑制了ATC细胞的增殖；IC50值范围为1.99至9.97纳摩尔。将紫杉醇封装到纳米药物载体中可以提高其水溶性、选择性地传递给癌细胞、组织毒性、控制释放和药代动力学特性，从而改善其对人体的毒性，保持或增强其活性并改善其药代动力学特性。在 vitro 实验中，在短时间内接触紫杉醇可诱导 IkappaB-alpha 的磷酸化和降解，进而导致 NF-kappaB 在人乳腺癌BCap37和人表皮样癌KB细胞中被激活。此外，通过将紫杉醇加载到自体前列腺癌细胞衍生的EVs上可以增强其细胞毒作用。
在体内实验中，使用1毫克/千克和20毫克/千克紫杉醇治疗后，低剂量紫杉醇处理的小鼠肝脏中浅色斑点转移显著增加，而高剂量紫杉醇组的转移明显减少。在体内，C643细胞来源的异种移植瘤在接受5毫克/千克口服利妥昔单抗和5毫克/千克腹腔注射紫杉醇处理组中生长速度较缓慢，比对照组要慢。
| Cell experiment [1]: | |
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Cell lines |
MCF-7 and MDA-MB-231 human breast carcinoma cell lines |
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Preparation Method |
The cells were transiently transfected with p21 promoter-luciferase reporter constructs using Lipofectamine, as recommended by the manufacturer. Following transfection, the cells were incubated for 12 h, the medium was exchanged, and the cells were incubated for various periods of time in the presence of 20 nM Paclitaxel . |
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Reaction Conditions |
20 nM; 12h |
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Applications |
The untreated control cells displayed exponential growth during the 48-h incubation, whereas paclitaxel (taxol) treatment resulted in a dramatic decrease in the number of viable cells. |
| Animal experiment [2]: | |
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Animal models |
Specific pathogen free nude mice |
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Preparation Method |
MDA-231 cells (1 × 106) were subcutaneously transplanted. After the formation of primary tumors (diameter > 5 mm), the mice were randomly grouped (10 mice per group) and 1 mg/kg paclitaxel were diluted with normal saline and administrated by intraperitoneal injection (1 time/2 days). |
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Dosage form |
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Applications |
Paclitaxel (1 mg/kg, i.p.) induces changes in estrogen metabolism in liver that facilitate the formation of breast cancer metastases. |
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References: [1]. [1]Choi YH, Yoo YH. Taxol-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]. 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. |
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| Cas No. | 33069-62-4 | SDF | |
| 别名 | 紫杉醇 | ||
| Canonical SMILES | O=C(N[C@H]([C@H](C(O[C@H]1C[C@]2(O)C(C)(C)C([C@@H](OC(C)=O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@H]4C[C@@H]3O)([H])[C@@H]2OC(C5=CC=CC=C5)=O)=O)=C1C)=O)O)C6=CC=CC=C6)C7=CC=CC=C7 | ||
| 分子式 | C47H51NO14 | 分子量 | 853.91 |
| 溶解度 | ≥ 42.6955mg/mL in DMSO, ≥ 31.6 mg/mL in EtOH with ultrasonic | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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