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Nocodazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nocodazole图片
CAS NO:31430-18-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
诺考达唑
Oncodazole
R17934
产品介绍
Nocodazole (Oncodazole) 是快速可逆的microtubule抑制剂。 Nocodazole与β-微管蛋白结合并破坏微管组装/拆卸动力学,从而防止有丝分裂并诱导肿瘤细胞凋亡。Nocodazole 抑制Bcr-Abl,增强CRISPR/Cas9的活性。
生物活性

Nocodazole (Oncodazole) is a rapidly-reversible inhibitor ofmicrotubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and inducesapoptosisin tumor cells. Nocodazole inhibitsBcr-Abl, and activatesCRISPR/Cas9.

IC50& Target[1]

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 Kdvalue 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)[1]. Nocodazole has the highest affinity for αβIVand the lowest affinity for αβIII[2].
Nocodazole (1 nM) induces apoptosis of COLO 205 cancer cells[3].
Nocodazole (≥ 30 μg/mL) significantly increases the percentage of annexin-V-binding cells without significantly modifying average forward scatter of human erythrocytes[4].
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[6].

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[3].

分子量

301.32

性状

Solid

Formula

C14H11N3O3S

CAS 号

31430-18-9

中文名称

诺考达唑

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.3187 mL16.5937 mL33.1873 mL
5 mM0.6637 mL3.3187 mL6.6375 mL
10 mM0.3319 mL1.6594 mL3.3187 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.

    请依序添加每种溶剂: 50%PEG300   50% saline

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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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
*以上所有助溶剂都可在本网站选购。