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ZM 447439
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
CAS No. 331771-20-1
文献中Selleckの製品使用例（67）
製品安全説明書
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純度：
99.26%
99.26
ZM 447439関連製品
シグナル伝達経路
Aurora Kinase阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| human LoVo cells | Proliferation assay | 72 h | Antiproliferative activity against human LoVo cells after 72 hrs by MTT-based WST8 reagent assay, IC50=1.9 μM | 25270403 | |
| MCF7 cell | Proliferation assay | Antiproliferative activity against MCF7 cell line, IC50=0.198 μM | 16337122 | ||
| human EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.18678 μM | SANGER | ||
| human P12-ICHIKAWA cell | Growth inhibition assay | Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=0.22441 μM | SANGER | ||
| human KARPAS-45 cell | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.38128 μM | SANGER | ||
| human ES3 cell | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50=0.4732 μM | SANGER | ||
| human ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.49806 μM | SANGER | ||
| human TE-11 cell | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50=0.53703 μM | SANGER | ||
| human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.5544 μM | SANGER | ||
| human MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=0.60961 μM | SANGER | ||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=0.70656 μM | SANGER | ||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.7963 μM | SANGER | ||
| human SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.83635 μM | SANGER | ||
| human BE-13 cell | Growth inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.84418 μM | SANGER | ||
| human MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=0.89978 μM | SANGER | ||
| human NBsusSR cell | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=0.91387 μM | SANGER | ||
| human H9 cell | Growth inhibition assay | Inhibition of human H9 cell growth in a cell viability assay, IC50=0.92979 μM | SANGER | ||
| human A172 cell | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50=0.98411 μM | SANGER | ||
| human ES5 cell | Growth inhibition assay | Inhibition of human ES5 cell growth in a cell viability assay, IC50=1.00248 μM | SANGER | ||
| human SBC-1 cell | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=1.03928 μM | SANGER | ||
| human NCI-H209 cell | Growth inhibition assay | Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=1.16602 μM | SANGER | ||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.16798 μM | SANGER | ||
| human NCI-H720 cell | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=1.20627 μM | SANGER | ||
| human KE-37 cell | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=1.21388 μM | SANGER | ||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=1.23155 μM | SANGER | ||
| human IST-SL1 cell | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=1.31727 μM | SANGER | ||
| human SK-NEP-1 cell | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=1.36498 μM | SANGER | ||
| human NOMO-1 cell | Growth inhibition assay | Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=1.36725 μM | SANGER | ||
| human DOHH-2 cell | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.40276 μM | SANGER | ||
| human ABC-1 cell | Growth inhibition assay | Inhibition of human ABC-1 cell growth in a cell viability assay, IC50=1.40352 μM | SANGER | ||
| human Ramos-2G6-4C10 cell | Growth inhibition assay | Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.40605 μM | SANGER | ||
| human EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=1.41721 μM | SANGER | ||
| human NB14 cell | Growth inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50=1.55621 μM | SANGER | ||
| human MOLT-13 cell | Growth inhibition assay | Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=1.56706 μM | SANGER | ||
| human ECC10 cell | Growth inhibition assay | Inhibition of human ECC10 cell growth in a cell viability assay, IC50=1.63353 μM | SANGER | ||
| human LK-2 cell | Growth inhibition assay | Inhibition of human LK-2 cell growth in a cell viability assay, IC50=1.64594 μM | SANGER | ||
| human CTB-1 cell | Growth inhibition assay | Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=1.67082 μM | SANGER | ||
| human NCI-H1581 cell | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=1.6755 μM | SANGER | ||
| human COLO-800 cell | Growth inhibition assay | Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=1.70382 μM | SANGER | ||
| human NB7 cell | Growth inhibition assay | Inhibition of human NB7 cell growth in a cell viability assay, IC50=1.75297 μM | SANGER | ||
| human LAMA-84 cell | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=1.7552 μM | SANGER | ||
| human HCT-116 cells | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=1.80908 μM | SANGER | ||
| SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=1.8153 μM | SANGER | ||
| human H4 cell | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50=1.81578 μM | SANGER | ||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=1.83845 μM | SANGER | ||
| human HN cell | Growth inhibition assay | Inhibition of human HN cell growth in a cell viability assay, IC50=1.9251 μM | SANGER | ||
| human L-363 cell | Growth inhibition assay | Inhibition of human L-363 cell growth in a cell viability assay, IC50=1.9512 μM | SANGER | ||
| human NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=2.03353 μM | SANGER | ||
| human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=2.3669 μM | SANGER | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | An Aurora selective ATP-competitive inhibitor. | ||||||||||
| Targets |
|
| In Vitro | ||||
| In vitro | 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] | |||
|---|---|---|---|---|
| Kinase Assay | 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. | ||||
| 細胞実験 | 細胞株 | BON, QGP-1 and MIP-101 cells | ||
| 濃度 | 0-5 μM | |||
| 反応時間 | 72 hours | |||
| 実験の流れ | 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. | |||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p53 / p21 / p-p38 / p38 pHistone H3 / CEM BubR1 / MAD2 / Cyclin B1 |
|
23759594 | |
| Immunofluorescence | p21 p53 Aurora B / Survivin |
|
23759594 | |
化学情報
| 分子量 | 513.59 | 化学式 | C29H31N5O4 |
| CAS No. | 331771-20-1 | SDF | Download ZM 447439 SDFをダウンロードする |
| Smiles | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)NC(=O)C4=CC=CC=C4)OCCCN5CCOCC5 | ||
| 保管 | |||
|
In vitro |
DMSO : 103 mg/mL ( (200.54 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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