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Nocodazole (Synonyms: 诺考达唑; Oncodazole; R17934)
目录号: PC16218 纯度: ≥98%
CAS No. :31430-18-9
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PC16218-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥539.00 请登录
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中文名称
Nocodazole
中文别名
诺考达唑;甲基-(5-[2 - 噻吩羰基]-1H-苯并咪唑-2-基)氨基甲酸酯;1H-苯并[D]咪唑-6-甲酰胺;诺考哒唑;[5-(2-噻吩羰基)-1H-苯并咪唑-2-基]氨基甲酸甲酯
英文名称
Nocodazole
英文别名
NOCODAZOLE;[5-(2-THIENYLCARBONYL)-1H-BENZIMIDAZOL-2-YL]CARBONIC ACID, METHYL ESTER;METHYL[5-(2-THIENYLCARBONYL)-1H-BENZIMADAZOL-2-YL]CARBAMATE;METHYL-(5-[2-THIENYLCARBONYL]-1H-BENZIMIDAZOL-2-YL)CARBAMATE;METHYL [5-(2-THIENYLCARBONYL)-1H-BENZ-IMIDAZOLE-2-YL]-CARBAMATE;METHYL-(5-[2-THIENYLCARBONYL]-1H-BENZIMODAZOL-2YL)-CARBAMATE;METHYL N-(5-THENOYL-2-BENZIMIDAZOLYL)CARBAMATE;R 17934;Methyl [5-(2-thienylcarbonyl)-1H-benzimidazol-2-yl]carbamate;methyl N-[6-(thiophene-2-carbonyl)-1H-benzimidazol-2-yl]carbamate;Methyl-(5-[2-thienylcarbonyl]-1H-benzimidazol-2yl)carbamate;Nocodazole (NSC 238159, R 17934, Oncodazole);methyl 5-(thiophene-2-carbonyl)-1H-benzo[d]imidazol-2-ylcarbamate;Nocidazole;Nocodazol;Nocodazolum;Oncodazole;[5-(2-Thienylcarbonyl)-1H-benzimidazol-2-yl]-carbamic acid methyl ester;[5-(2-Thienylcarbonyl)-1H-benzimidazol-2-yl]carbamic Acid Methyl Ester
Cas No.
31430-18-9
分子式
C14H11N3O3S
分子量
301.32
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.

性状

Solid

IC50 & Target[1][2]

Abl

91 nM (Kd)

ABL(E255K)

120 nM (Kd)

ABL(T315I)

170 nM (Kd)

BRAF

1.8 μM (Kd)

BRAF(V600E)

1.1 μM (Kd)

c-KIT

1.6 μM (Kd)

MEK1

1.7 μM (Kd)

MEK2

1.6 μM (Kd)

MET

1.7 μM (Kd)

PI3Kγ

1.5 μM (Kd)

Microtubule/Tubulin

 

CRISPR/Cas9

 

体外研究(In Vitro)

Nocodazole exhibits good affinity toward c-KIT, with a Kd value of 1.6?μM in highly malignant human cancer cells. Nocodazole displays good binding affinity toward the components of the mitogen-activated protein kinase (MAPK) pathway, such as BRAF (Kd=1.8?μM), BRAF(V600E) (Kd=1.1?μM), MEK1 (Kd=1.7?μM), and MEK2 (Kd=1.6?μM). Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII.
Nocodazole (1 nM) induces apoptosis of COLO 205 cancer cells.
Nocodazole (≥ 30 μg/mL) significantly increases the percentage of annexin-V-binding cells without significantly modifying average forward scatter of human erythrocytes.
In CHO cells, the addition of 1 nM Nocodazole, a concentration that suppresses microtubule dynamics, slows migration and increases the frequency and duration of resting states, but the directionality of the cells is maintained. In contrast to the effects of the low drug concentration, the addition of 70 nM Nocodazole, a concentration that eliminates the microtubule network, causes cells to move much more randomly, i.e., the directionality of the cells toward the wound is lost.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Nocodazole (5 mg/kg/three times per week, i.p.) has antitumor effects in athymic mice bearing COLO 205 tumor xenografts. Nocodazole (1 nM) + R-41400 dramatically increase the levels of p21/CIP1 and p27/KIP1 protein in the tumor tissues.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 20 mg/mL (66.37 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 5 mg/mL (16.59 mM); Suspended solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (6.64 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (6.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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