Paclitaxel 紫杉醇
| EC | EINECS 205-285-7 |
| MDL | MFCD00869953 |
| 别名 | Paxene; Taxol A; LipoPac; Ebetaxel; ABI 007 |
| CAS | 33069-62-4 |
| 分子式 | C47H51NO14 |
| 分子量 | 853.92 |
| 纯度 | HPLC≥98% |
| 单位 | 瓶 |
| 生物活性 | Paclitaxel是一种有效的抗癌药物的主要成分, 可以促进微管 (microtubule (MT) ) 组装, 抑制MT解聚, 并改变有丝分裂和细胞增殖所需的微管动力学[1-6]。 |
| IC50 | IC50: 4 nM (MT) [1-6] |
| In Vitro | 0.1, 0.5和1μM的紫杉醇以剂量依赖的方式降低CCRF-HSB-2细胞的增殖和存活, 并且紫杉醇的IC50值约为0.25μM[1]。紫杉醇直接与内质网结合, 刺激钙释放到细胞质中, 有助于诱导细胞凋亡[2]。 |
| In Vivo | 在SCID小鼠异种移植模型中, 低剂量节律性紫杉醇治疗可减少EGI-1细胞的肺传播, 而不会显着影响其局部肿瘤生长。低剂量的紫杉醇促进小鼠异种移植物中的肝转移, 这与宿主肝脏中雌激素代谢的变化相关。 |
| 激酶实验 | 为了确定哪种半胱天冬酶参与紫杉醇, 半胱天冬酶-3抑制剂 (DEVD-CHO) , 半胱天冬酶-6抑制剂 (Z-VEID-FMK) , 半胱天冬酶-8抑制剂 (Z-IETD-FMK或IETD-CHO) 诱导的细胞凋亡, 使用胱天蛋白酶-9抑制剂 (Z-LEHD-FMK或LEHD-CHO) 和半胱天冬酶-10抑制剂 (Z-AEVD-FMK) 。将这些半胱天冬酶抑制剂溶于二甲基亚砜 (Me2SO) 中; Me2SO的最终浓度为0.1％。将细胞 (5×105) 在存在或不存在100μM这些抑制剂的情况下于37℃预孵育3小时, 然后用或不用0.1, 0.5和1μM紫杉醇处理48小时并处理用于膜联蛋白V结合测定。 |
| SMILES | O=C(C1=CC=CC=C1)N[C@@H](C2=CC=CC=C2)[C@H](C(O[C@@H]3C(C)=C([C@@H](OC(C)=O)C([C@@]4(C)[C@]([C@@](CO5)(OC(C)=O)[C@@]5([H])C[C@@H]4O)([H])[C@@H]6OC(C7=CC=CC=C7)=O)=O)C(C)(C)[C@@]6(O)C3)=O)O |
| 靶点 | Microtubule/Tubulin |
| 动物实验 | 以MDA-231异种移植小鼠[4]为研究对象，紫杉醇（1-20 mg / kg；腹腔注射； 1次/ 2天，连续5个周期）处理。 |
| 细胞实验 | 在存在或不存在浓度增加的 (0.1-1μM) 紫杉醇的96孔板中将1×10 4个细胞接种在100μL生长培养基中, 并在37℃, 5％CO 2中培养12-48小时。然后将细胞与25μLMTT (5mg / mL) 在37℃下孵育4小时。用0.04N HCl的异丙醇溶解晶体后, 在酶标仪中在570nm处读板。从细胞存活图确定抑制细胞存活50％ (IC50) 的药物浓度。 |
| 数据来源文献 | [1]. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3; 279 (49) :51057-67. Epub 2004 Sep 27. [2]. 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. [3]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21. [4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16. [5]. 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. [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. |
| 备注 | 以上数据均来自公开文献, Jinpan暂未进行独立验证, 仅供参考。These protocols are for reference only. Jinpan does not independently validate these methods. |
| 规格 | 10mg 10mM*1mL (in DMSO) 50mg |
紫杉醇可使微管蛋白和组成微管的微管蛋白二聚体失去动态平衡，诱导与促进微管蛋白聚合、微管装配、防止解聚，从而使微管稳定并抑制癌细胞的有丝分裂和防止诱导细胞凋亡，进而有效阻止癌细胞的增殖，起到抗癌作用。
使用本产品的应用案例（仅供参考）
In Vitro:
细胞实验：Cytotoxicity determination: The IC50 of cells exposed to PTX was determined using a Cell Counting Kit (CCK)‑8 assay. In brief, cells were inoculated at a concentration of 4×103/100 µl per well and cultured at 37˚C for 12 h in a 96‑well plate. The cells were then maintained at 37˚C with 200 µl fresh medium containing different concentrations of PTX (0‑50 nM) for 48 h. Following this, the cells were incubated with 20 µl CCK‑8 solution at 37˚C for 24 h. Then, the optical density value of each well was detected using a microplate reader at 450 nm.
ROS检测：For ROS detection, 5×105 cells were seeded overnight in a 6‑well plate and then treated with PTX (5 nM) at 37˚C for 48 h. Subsequently, 5 µM carboxy 2'‑7'‑dichlorofluorescein diacetate was added in Hanks' Balanced Salt Solution and incubated with cells at room temperature for 0.5 h. Fresh tissues were harvested, followed by a single cell suspension preparation. Tissue was digested with trypsin to obtain single cell suspension. Cells were then inoculated in a 6‑well plate as aforementioned. The levels of intracellular peroxide were measured using a flow cytometer at 485 nm excitation and 520 nm emission to analyze the ROS generation.
来源文献：Chen M, Su J, Feng C, Liu Y, Zhao L, Tian Y. Chemokine CCL20 promotes the paclitaxel resistance of CD44+CD117+cells via the Notch1 signaling pathway in ovarian cancer. Mol Med Rep. 2021 Sep;24(3):635. doi: 10.3892/mmr.2021.12274. Epub 2021 Jul 19. PMID: 34278466; PMCID: PMC8280726.
In Vivo：
小鼠，腹腔注射：Xenograft and grouping：In total, 16 male nude mice (age, 6‑8 weeks; weight, 25‑30 g) . Mice were housed at 25±1˚C with 12‑h light/dark cycles, 50±5% humidity and free access to food and water. The mice were randomly divided into four groups: i) CD44+CD117++ PTX (Beijing Jinpan Science & Technology Co., Ltd.) group (n=4); ii) CD44+CD117++ PTX + CCL20 (Beijing Jinpan Science & Technology Co., Ltd.) group (n=4); iii) CD44‑CD117‑+ PTX group (n=4); and iv) CD44‑CD117‑ + PTX + CCL20 group (n=4). For xenografts, CD44+CD117+(2×106) subsets or CD44‑CD117‑subsets cells (2×106) suspended in 0.5 ml PBS were subcutaneously injected into the left flank of each nude mouse to establish tumors. Then, PTX (10 mg/kg) and/or CCL20 (1 mg/kg) were injected intraperitoneally simultaneously on days 1, 3 and 7. Tumor size was monitored on the 3rd, 7th, 14th, 21st and 28th days (15). At the end of the experiment and under continuous anesthesia, the animals were euthanized by an overdose of pentobarbital (125 mg/kg).
来源文献：Chen M, Su J, Feng C, Liu Y, Zhao L, Tian Y. Chemokine CCL20 promotes the paclitaxel resistance of CD44+CD117+cells via the Notch1 signaling pathway in ovarian cancer. Mol Med Rep. 2021 Sep;24(3):635. doi: 10.3892/mmr.2021.12274. Epub 2021 Jul 19. PMID: 34278466; PMCID: PMC8280726.