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Purity: ≥98%
Nocodazole (Oncodazole; R-17934; R17934) is a potent and rapidly-reversible inhibitor of microtubule polymerization/microtubule destablizer, the so called antimitotic or antitubulin agent, with potential antineoplastic activity. It also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole is used as an anti-cancer agent which exerts its effect in cells by interfering with the polymerization of microtubules. Nocodazole induces apoptosis in chronic lymphocytic leukemia cells. It inhibits insulin-stimulated glucose transport. Nocodazole decreases apoptosis in some human colon carcinoma cells.
| ln Vitro |
In highly aggressive human cancer cells, nocodazole has a Kd value of 1.6 μM, indicating excellent affinity toward c-KIT. The mitogen-activated protein kinase (MAPK) pathway's constituents, including BRAF (Kd=1.8 μM), BRAF(V600E) (Kd=1.1 μM), MEK1 (Kd=1.7 μM), and MEK2 (Kd=1.6 μM), are well-bound by nocodazole[1]. Nocodazole promotes apoptosis in COLO 205 cancer cells at a concentration of 1 nM. It has the highest affinity for αβIV and the lowest affinity for αβIII[2]. The fraction of annexin-V-binding cells is dramatically increased by nocodazole (≥ 30 µg/mL) without appreciably altering the average forward scatter of human erythrocytes[4]. CHO cells are exposed to 1 nM nocodazole, a dose that inhibits microtubule dynamics, delays migration, and lengthens and increases the frequency of resting states while maintaining the directionality of the cells. The application of 70 nM Nocodazole, a concentration that destroys the microtubule network, reverses the effects of the low drug concentration and causes cells to migrate considerably more randomly, losing their directionality toward the wound[6].
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| ln Vivo |
Athymic mice with COLO 205 tumor xenografts have anticancer effects in response to nocodazole (5 mg/kg/three times per week, ip). The amounts of p21/CIP1 and p27/KIP1 protein in the tumor tissues are markedly increased by nocodazole (1 nM) + R-41400[3].
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| References |
[1]. Park H, et al. Nocodazole is a high-affinity ligand for the cancer-related kinases ABL, c-KIT, BRAF, and MEK. ChemMedChem. 2012 Jan 2;7(1):53-6.
[2]. Keliang Xu, et al. Interaction of nocodazole with tubulin isotypes. Drug Development Research 2002 [3]. Wang YJ, et al. R-41400 potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice. Mol Carcinog. 2002 Aug;34(4):199-210. [4]. Signoretto E, et al. Nocodazole Induced Suicidal Death of Human Erythrocytes. Cell Physiol Biochem. 2016;38(1):379-92. [5]. Zhang JP, et al. Efficient precise knockin with a double cut HDR donor after CRISPR/Cas9-mediated double-stranded DNA cleavage. Genome Biol. 2017 Feb 20;18(1):35. [6]. Anutosh Ganguly, et al. The role of microtubules and their dynamics in cell migration. J Biol Chem. 2012 Dec 21;287(52):43359-69 |
| Molecular Formula |
C14H11N3O3S
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| Molecular Weight |
301.32
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| CAS # |
31430-18-9
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| Related CAS # |
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| SMILES |
O=C(OC)NC1=NC2=CC=C(C(C3=CC=CS3)=O)C=C2N1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 1% DMSO +30% polyethylene glycol+1% Tween 80 :30 mg/mL Solubility in Formulation 4: 5 mg/mL (16.59 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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