ZM 447439

ZM 447439は、オーロラ選択ATPです-競争的な阻害剤で、オーロラAキナーゼとオーロラBキナーゼに作用すると、IC50が それぞれ 110 nM と 130 nM,になる。

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ZM 447439 化学構造
分子量: 513.59



Quality Control & MSDS


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情報 ZM 447439は、オーロラ選択ATPです-競争的な阻害剤で、オーロラAキナーゼとオーロラBキナーゼに作用すると、IC50が それぞれ 110 nM と 130 nM,になる。
目標 Aurora A Aurora B
IC50 110 nM 130 nM [1]
In vitro試験 In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. [1] Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle. [2] In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle. [3] A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin. [4]
In vivo試験
特集 An Aurora selective ATP-competitive inhibitor.

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

In vitro kinase assays Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. 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 BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen.

細胞アッセイ: [2]

細胞系 BON, QGP-1 and MIP-101 cells
濃度 0-5 μM
処理時間 72 hours
方法 Cell number is evaluated by crystal violet staining. In brief, cells in 96-well plates are fixed with 1% glutaraldehyde. Then cells are stained with 0.1% crystal violet. The unbound dye is removed by washing with water. Bound crystal violet is solubilized with 0.2% Triton X-100. Light extinction which increases linearly with the cell number is analyzed at 570 nm using an ELISA reader.



Download ZM 447439 SDF
分子量 513.59


CAS No. 331771-20-1
保管 2年-20℃
6月-80℃in DMSO
溶解度 (25°C) * In vitro DMSO 103 mg/mL (200 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(4-(6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-ylamino)phenyl)benzamide


カスタマーレビュー (3)

Click to enlarge
Source Mol Biol Cell, 2011, 22(22), 4227-35. ZM 447439 purchased from Selleck
Method Flow cytometry
Cell Lines HeLa Tet-on cells
Incubation Time 0-1 h
Results p31comet depletion did not block mitotic exit induced by Aurora B inhibitor ZM447439.

Click to enlarge
Source Dr Yuanhong Chen of University of Nebraska. ZM 447439 purchased from Selleck
Method Western blot
Cell Lines HeLa cells
Concentrations 1 μM
Incubation Time 2 h
Results The results showed that ZM447439 inhibits both Aurora-B and –C kinases, but not Aurora-A kinase.

Click to enlarge
Source Dr. Zhang of Tianjin Medical University. ZM 447439 purchased from Selleck
Method Western blot
Cell Lines
Concentrations 0-10 μM
Incubation Time
Results ZM447439 treatment resulted in a reduction of Histone H3 and Aurora A/B/C phosphorylation.

製品表彰状 (7)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


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