Nocodazole
(Synonyms: 诺考达唑) 目录号 : GC14075
Nocodazole是一种抗有丝分裂药物，是一种快速可逆的微管聚合抑制剂，在无细胞试验中抑制Abl，Abl（E255K）和Abl（T315I），IC50值分别为0.21μM，0.53μM和0.64μM。
Cas No.:31430-18-9
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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| Cell experiment [1]: | |
Cell lines | HuH7 cells |
Preparation Method | HuH7 cells were grown in Dulbecco's modified Eagle's medium supplemented with 10 % fetal bovine serum, 100 U/ml penicillin, and 100 μg/ml streptomycin at 37 °C in 5 % CO2 incubator. To synchronize the cells at prometaphase, they were treated with 50 ng/ml nocodazole for 16 h. |
Reaction Conditions | 50 ng/ml; 16h |
Applications | Approximately 50 % of the cells were synchronized in G2/M phases. |
| Animal experiment [2]: | |
Animal models | nude mouse |
Preparation Method | COLO 205 cells were injected subcutaneously between the scapulae of each nude mouse. Once tumors reached a mean size of 200mm3 , animals received intraperitoneal injections of DMSO (25µL), ketoconazole(50 mg/kg), nocodazole(5 mg/kg), or ketoconazole+nocodazole three times per week for 6 week. |
Dosage form | 5mg/kg; i.p. |
Applications | Nocodazole has antitumor effects in athymic mice bearing COLO 205 tumor xenografts. |
References: [1]Makiyama T, Obama T, Watanabe Y, et al. Behavior of intracellular lipid droplets during cell division in HuH7 hepatoma cells[J]. Experimental Cell Research, 2023, 433(2): 113855. [2]Wang Y J, Jeng J H, Chen R J, et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice[J]. Molecular Carcinogenesis: Published in cooperation with the University of Texas MD Anderson Cancer Center, 2002, 34(4): 199-210. | |
Nocodazole is an anti-mitotic drug and a rapid and reversible microtubule polymerization inhibitor. It inhibits Abl, Abl (E255K), and Abl (T315I) in cell-free assays with IC50 values of 0.21μM, 0.53μM, and 0.64μM, respectively[1]. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, thereby arresting mitosis and inducing apoptosis in tumor cells[2]. Nocodazole can increase CRISPR-mediated homologous recombination efficiency, enhancing the precision of gene editing efficacy[3].
In vitro, Nocodazole (50 ng/ml) treatment of HuH7 cells for 16 hours synchronizes approximately 50% of the cells at the G2/M phase, with intracellular microtubule fibers mainly distributed in the peripheral region of the cells and without forming a bipolar spindle[4]. Nocodazole (20µM) treatment of emsCOS-1 cells for 30 minutes results in the dispersion of Golgi stacks throughout the cytoplasm[5]. Nocodazole (1 nM) treatment of CHO cells inhibits microtubule dynamics, slowing migration and increasing the frequency and duration of the resting state while maintaining cell directionality. Nocodazole (70nM) has the opposite effect of low drug concentrations, causing cells to move more randomly[6].
In vivo, Nocodazole (5 mg/kg) administered intraperitoneally for six weeks significantly reduces the tumor volume and weight in mice transplanted with COLO 205 tumors, with enhanced antitumor effects observed when combined with ketoconazole[7].
References:
[1] Park H, Hong S. Nocodazole is a high-affinity ligand for the cancer-related kinases ABL, c-KIT, BRAF, and MEK[J]. ChemMedChem, 2011, 7(1): 53-56.
[2] Jordan M A, Wilson L. Microtubules and actin filaments: dynamic targets for cancer chemotherapy[J]. Current opinion in cell biology, 1998, 10(1): 123-130.
[3] Chen S, Chen D, Liu B, et al. Modulating CRISPR/Cas9 genome-editing activity by small molecules[J]. Drug Discovery Today, 2022, 27(4): 951-966.
[4] Makiyama T, Obama T, Watanabe Y, et al. Behavior of intracellular lipid droplets during cell division in HuH7 hepatoma cells[J]. Experimental Cell Research, 2023, 433(2): 113855.
[5] Mukai, K., Konno, H., Akiba, T. et al. Activation of STING requires palmitoylation at the Golgi[J]. Nat Commun 7, 11932 (2016).
[6] Ganguly A, Yang H, Sharma R, Patel KD, Cabral F. The role of microtubules and their dynamics in cell migration[J]. J Biol Chem. 2012, 287(52):43359-69.
[7] Wang Y J, Jeng J H, Chen R J, et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice[J]. Molecular Carcinogenesis: Published in cooperation with the University of Texas MD Anderson Cancer Center, 2002, 34(4): 199-210.
Nocodazole是一种抗有丝分裂药物，是一种快速可逆的微管聚合抑制剂，在无细胞试验中抑制Abl，Abl（E255K）和Abl（T315I），IC50值分别为0.21μM，0.53μM和0.64μM[1]。Nocodazole与β-微管蛋白结合并破坏微管组装/拆卸动力学，从而阻止有丝分裂并诱导肿瘤细胞凋亡[2]。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用[3]。
在体外，Nocodazole（50 ng/ml）处理HuH7细胞16h，使大约50%的细胞同步于G2/M期，细胞内微管蛋白纤维主要分布在细胞的外围区域，并且没有形成双极纺锤体[4]。Nocodazole（20µM）处理emsCOS-1细胞30min，会导致细胞质中分散的高尔基体堆栈[5]。Nocodazole（1nM）处理CHO细胞，可抑制微管动力学，减缓迁移并增加静息状态的频率和持续时间，但细胞的方向性得以保持。Nocodazole（70nM）与低药物浓度的影响相反，会导致细胞更加随机地移动[6]。
在体内，Nocodazole（5mg/kg）通过腹腔注射治疗移植了COLO 205肿瘤的小鼠6周，显著减小了肿瘤体积和重量，且在酮康唑的联合治疗下抗肿瘤效应增强[7]。
| Cas No. | 31430-18-9 | SDF | |
| 别名 | 诺考达唑 | ||
| 化学名 | methyl N-[6-(thiophene-2-carbonyl)-1H-benzimidazol-2-yl]carbamate | ||
| Canonical SMILES | COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CS3 | ||
| 分子式 | C14H11N3O3S | 分子量 | 301.32 |
| 溶解度 | ≥ 15.1mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 3.3187 mL | 16.5937 mL | 33.1873 mL |
| 5 mM | 0.6637 mL | 3.3187 mL | 6.6375 mL |
| 10 mM | 0.3319 mL | 1.6594 mL | 3.3187 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。