ZM-447439
Based on 7 publication(s) in Google Scholar
ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.55%
- CAS. Nr.: 331771-20-1
- Formel: C29H31N5O4
- Molecular Weight:513.59
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ZM-447439
MoreAlle Aurora Kinase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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Aurora A 110 nM (IC50) |
Aurora B 130 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.3 μM
Compound: ZM447439
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Antiproliferative activity against human A549 cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
| HepG2 | IC50 |
1.4 μM
Compound: ZM447439
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Antiproliferative activity against human HepG2 cells after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human HepG2 cells after 72 hrs by sulforhodamine B assay
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[PMID: 28279846] |
| HT-29 | IC50 |
2.2 μM
Compound: ZM447439
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Antiproliferative activity against human HT-29 cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
| K562 | IC50 |
>100 μM
Compound: ZM447439
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Antiproliferative activity against human K562 cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
| LoVo | IC50 |
1.9 μM
Compound: ZM447439
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Antiproliferative activity against human LoVo cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human LoVo cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
| MCF7 | IC50 |
198 nM
Compound: 2
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Antiproliferative activity against MCF7 cell line
Antiproliferative activity against MCF7 cell line
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[PMID: 16337122] |
| NCI-H661 | IC50 |
2.9 μM
Compound: ZM447439
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Antiproliferative activity against human NCI-H661 cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human NCI-H661 cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
| U-937 | IC50 |
>100 μM
Compound: ZM447439
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Antiproliferative activity against human U937 cells after 72 hrs by MTT-based WST8 reagent assay
Antiproliferative activity against human U937 cells after 72 hrs by MTT-based WST8 reagent assay
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[PMID: 25270403] |
Cells treated with ZM-447439 progress through interphase, enter mitosis normally, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and inhibit mitotic phosphorylation of histone H3. ZM-447439 prevents chromosome alignment and segregation. ZM-447439 compromises spindle checkpoint function. ZM-447439 inhibits kinetochore localization of BubR1, Mad2, and Cenp-E[1]. Inhibition of Aurora kinase by ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinoma cells. Multipolar spindles are induced in these ZM-treated G2/M-arrested cells with accumulation of 4N/8N DNA, similar to cells with genetically suppressed Aurora-B. ZM-447439 treatment induces cell apoptosis. ZM-447439 inhibition of Aurora kinase is potently in association with decrease of Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 331771-20-1
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Appearance Solid
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Molecular Weight 513.59
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Formel C29H31N5O4
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Color White to gray
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SMILES
O=C(NC1=CC=C(NC2=C(C(C=C3OCCCN4CCOCC4)=NC=N2)C=C3OC)C=C1)C5=CC=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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EBioMedicine
Transcriptomics based multi-dimensional characterization and drug screen in esophageal squamous cell carcinoma. [Abstract]2021 Aug:70:103510. PMID: 34365093 -
EMBO J
2024 Nov;43(22):5381-5420. PMID: 39327527 -
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bioRxiv
2024 Dec 5:2024.12.05.627000. PMID: 39677682 -
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Elife
2020 Dec 7:9:e61405. PMID: 33284104
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (48.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
1 ng purified recombinant enzyme is added to a reaction cocktail containing buffer, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ[33P]ATP, and is then incubated at room temperature for 60 min. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a Betaplate counter. No enzyme and no compound control values are used to determine the concentration of ZM-447439, which gave 50% inhibition of enzyme activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To determine cloning efficiency, MCF7 cells are plated in phenol red free DME plus 5% stripped serum, and are then treated with or without the anti-estrogen ICI 182780 at 1 μM for 48 h. ZM-447439 is then added at the indicated concentrations for 72 h. The cells are harvested, washed, and ∼400 cells plated in each well of a 6-well plate in complete media without ZM-447439. After 10 d, the colonies are fixed, stained with crystal violet, and counted. The cloning efficiency represents the number of colonies on ZM-447439-treated plates compared with DMSO-treated controls[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Ditchfield C, et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol. 2003 Apr 28;161(2):267-80. [Content Brief]
[2]. Long ZJ, et al. ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensionalculture. Cell Cycle. 2008 May 15;7(10):1473-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL | 48.6770 mL |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7354 mL | |
| 10 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL | 4.8677 mL | |
| 15 mM | 0.1298 mL | 0.6490 mL | 1.2981 mL | 3.2451 mL | |
| 20 mM | 0.0974 mL | 0.4868 mL | 0.9735 mL | 2.4338 mL | |
| 25 mM | 0.0779 mL | 0.3894 mL | 0.7788 mL | 1.9471 mL | |
| 30 mM | 0.0649 mL | 0.3245 mL | 0.6490 mL | 1.6226 mL | |
| 40 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2169 mL |
ZM-447439 Related Classifications
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