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Paclitaxel

Paclitaxel

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产品编号 T0968   CAS 33069-62-4
别名: Taxol, 紫杉醇, NSC 125973

Paclitaxel (Taxol) 属于天然产物,是一种微管聚合物稳定剂。Paclitaxel 具有抗肿瘤活性;通过诱导有丝分裂停滞、细胞凋亡、细胞自噬等,导致细胞死亡。

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Paclitaxel Chemical Structure
Paclitaxel, CAS 33069-62-4
规格 价格/CNY 货期 数量
1 mg ¥ 128 现货
5 mg ¥ 253 现货
10 mg ¥ 355 现货
25 mg ¥ 530 现货
50 mg ¥ 745 现货
100 mg ¥ 1,230 现货
500 mg ¥ 2,930 现货
1 mL * 10 mM (in DMSO) ¥ 461 现货
其他形式的 Paclitaxel:
618惊喜特惠 4重福利大放送
药物设计专题培训
产品目录号及名称: Paclitaxel (T0968)
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天然产物信息
生物活性
化学信息
存储 & 溶解度
TCMIP信息
参考文献
植物来源
天然产物 > 红豆杉科 > 红豆杉属 > Taxus chinensis
产品描述 Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.
靶点活性 Microtubule:4 nM
体外活性 方法:人 T 细胞淋巴细胞白血病细胞 CCRF-HSB-2 用 Paclitaxel (0.01-1 µM) 处理 48 h,使用 MTT 方法检测细胞生长抑制情况。
结果:Paclitaxel 剂量依赖性地抑制 CCRF-HSB-2 细胞生长,IC50 为 0.25 µM。[1]
方法:人胃癌细胞 AGS 用 Paclitaxel (10-160 nM) 处理 24-48 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Paclitaxel 诱导凋亡相关蛋白 cleaved caspase-3 和 cleaved PARP 表达上调。[2]
方法:犬乳腺肿瘤细胞 CHMm 用 Paclitaxel (0.01-1 μM) 处理 24 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:Paclitaxel 剂量依赖性诱导 CHMm 细胞凋亡。[3]
体内活性 方法:为研究低剂量 Paclitaxel 对肿瘤侵袭的影响,将 Paclitaxel (2.6 mg/kg) 腹腔注射给药给携带胆管癌肿瘤 EGI-1 的 SCID 小鼠,每天一次,持续两周。
结果:低剂量 Paclitaxel 治疗减少了 EGI-1 细胞的肺扩散,而不显著影响其局部肿瘤生长。[4]
方法:开发 Paclitaxel 醇诱导的负面情感症状的临床前模型,将 Paclitaxel (2-8 mg/kg in 1 volume ethanol+1 volume Emulphor-620 +18 volumes distilled water) 腹腔注射给 C57BL/6J 小鼠,每两天一次,共注射四次。
结果:8 mg/kg Paclitaxel 处理导致机械性和冷性异常性疼痛的发展和维持。Paclitaxel 也诱导了焦虑样行为和抑郁样行为。Paclitaxel 在小鼠情感状态建模试验中产生了行为改变,而伤害性反应的增加持续时间更长。[5]
激酶实验 To determine which caspases are involved in apoptosis induced by taxol, caspase-3 inhibitor (DEVD-CHO), caspase-6 inhibitor (Z-VEID-FMK), caspase-8 inhibitor (Z-IETD-FMK or IETD-CHO), caspase-9 inhibitors (Z-LEHD-FMK or LEHD-CHO), and caspase-10 inhibitor (Z-AEVD-FMK) are used. These caspase inhibitors are dissolved in dimethyl sulfoxide (Me2SO); the final concentration of Me2SO is 0.1%. Cells (5×105) are preincubated in the presence or absence of 100 μM?each of these inhibitors for 3 h at 37°C then treated with or without 0.1, 0.5, and 1 μM?Paclitaxel for 48 h and processed for annexin V binding assay [1].
细胞实验 1×10^4 cells are plated in 100 μL of the growth medium in the presence or absence of increasing concentrations (0.1-1 μM) of taxol in 96-well plates and cultured at 37°C in 5% CO2 for 12-48 h. The cells are then incubated with 25 μL of MTT (5 mg/mL) at 37°C for 4 h. After dissolving the crystals with 0.04 N HCl in isopropanol, the plates are read in a microplate reader at 570 nm [1].
动物实验 Adult (250-320 g) male Sprague-Dawley rats are used for all experiments. One week following the DiI injection, rats are anesthetized with isofluorane and injected into the tail vein with 2 mg/kg paclitaxel or its vehicle (1:1:23, cremophor EL:ethanol:0.9% saline). The tail vein injection is repeated three more times every other day for a total of four injections [4].
别名 Taxol, 紫杉醇, NSC 125973
分子量 853.91
分子式 C47H51NO14
CAS No. 33069-62-4

存储

keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 21.4 mg/mL (25 mM)

DMSO: 85.4 mg/mL (100 mM), Heating is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.1711 mL 5.8554 mL 11.7108 mL 29.2771 mL
5 mM 0.2342 mL 1.1711 mL 2.3422 mL 5.8554 mL
10 mM 0.1171 mL 0.5855 mL 1.1711 mL 2.9277 mL
20 mM 0.0586 mL 0.2928 mL 0.5855 mL 1.4639 mL
DMSO 50 mM 0.0234 mL 0.1171 mL 0.2342 mL 0.5855 mL
100 mM 0.0117 mL 0.0586 mL 0.1171 mL 0.2928 mL
TCMIP相关数据
中药材来源及性味归经

中药材来源及性味归经

中药材名称 中药材拉丁名 归经
短叶红豆杉 Taxus brevifolia -
海南粗榧 Cephalotaxus hainanensis Li【C.mannii Hook.f.】 苦, 涩
红豆杉 Taxus chinensis (Pilg.)Rehd. var. mairei (Lemee et Levl.)Cheng et L. K. Fu(T. speciosa Florin) -
酱果紫杉 Taxus baccata Linn. -
曼地亚红豆杉 Taxus × media -
美丽红豆杉 Taxus mairei (Lemée et Lévl.) S.Y.Hu -
喜马拉雅红豆杉 Taxus wallichiana Zucc. -
云南红豆杉 Taxus yunnanensis Cheng et L. K. Fu -
紫杉 Taxus cuspidata Sieb. et Zucc. -

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TargetMol Library Books参考文献

1. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. 2. Khing TM, et al. The effect of paclitaxel on apoptosis, autophagy and mitotic catastrophe in AGS cells. Sci Rep. 2021 Dec 6;11(1):23490. 3. Ren X, et al. Paclitaxel suppresses proliferation and induces apoptosis through regulation of ROS and the AKT/MAPK signaling pathway in canine mammary gland tumor cells. Mol Med Rep. 2018 Jun;17(6):8289-8299. 4. Cadamuro M, et al. Low-Dose Paclitaxel Reduces S100A4 Nuclear Import to Inhibit Invasion and Hematogenous Metastasis of Cholangiocarcinoma. Cancer Res. 2016 Aug 15;76(16):4775-84. 5. Toma W, et al. Effects of paclitaxel on the development of neuropathy and affective behaviors in the mouse. Neuropharmacology. 2017 May 1;117:305-315. 6. 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. 7. Sun J, Liu W, Li Y, et al. An on-chip cell culturing and combinatorial drug screening system[J]. Microfluidics and Nanofluidics. 2017 Jul 21(7): 125. 8. 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. 9. Pang G, Zhang S, Zhou X, et al. Immunoactive polysaccharide functionalized gold nanocomposites promote dendritic cell stimulation and antitumor effects[J]. Nanomedicine. 2019 May;14(10):1291-1306.

TargetMol Library Books文献引用

1. Gritsina G, Fong K, Lu X, et al.Chemokine receptor CXCR7 activates AURKA and promotes neuroendocrine prostate cancer growth.The Journal of Clinical Investigation.2023 2. Zhao X, Lian X, Xie J, et al.Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment.Redox Biology.2023: 102678. 3. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 4. Hou Z, Lin S, Du T, et al.S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer.Pharmaceuticals.2023, 16(5): 749. 5. Zhan Y, Chen Q, Song Y, et al. Berbamine Hydrochloride inhibits lysosomal acidification by activating Nox2 to potentiate chemotherapy-induced apoptosis via the ROS-MAPK pathway in human lung carcinoma cells. Cell Biology and Toxicology. 2022: 1-21 6. Pang G, Zhang S, Zhou X, et al. Immunoactive polysaccharide functionalized gold nanocomposites promote dendritic cell stimulation and antitumor effects. Nanomedicine. 2019 May;14(10):1291-1306 7. Sun J, Liu W, Li Y, et al. An on-chip cell culturing and combinatorial drug screening system. Microfluidics and Nanofluidics. 2017 Jul 21(7): 125. 8. ZeZhanga,b,c VLM catecholaminergic neurons control tumor growth by regulating CD8+ T cells. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA. 2020 9. Song X, Li D, Gan L, et al.Intravenous Injection of Na Ions Aggravates Ang II-Induced Hypertension-Related Vascular Endothelial Injury by Increasing Transmembrane Osmotic Pressure.International Journal of Nanomedicine.2023: 7505-7521. 10. Zeng L, Lyu X, Yuan J, et al.STMN1 Promotes Tumor Metastasis in Non-small Cell Lung Cancer Through Microtubule-dependent And Nonmicrotubule-dependent Pathways.International Journal of Biological Sciences.2024, 20(4): 1509.
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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Paclitaxel 33069-62-4 Antibody-drug Conjugate/ADC Related Apoptosis Autophagy Cytoskeletal Signaling ADC Cytotoxin Microtubule Associated Microtubule/Tubulin Inhibitor NSC-125973 Taxol 紫杉醇 ADC Payload NSC125973 inhibit NSC 125973 inhibitor

 

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