ZM 447439

製品コード：S1103 純度：99.26%

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

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 34000	国内在庫あり
25mg	JPY 55500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（72）

製品安全説明書

現在のバッチを見る：純度： 99.26%

99.26

ZM 447439関連製品

関連ターゲット	Aurora A Aurora B Aurora C Aurora B	もっと見る
関連製品	Alisertib (MLN8237) Barasertib (AZD1152-HQPA) Tozasertib (VX-680) MLN8054 Hesperadin Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 SNS-314 CCT137690 GSK1070916 CYC116 TAK-901 CCT129202 SNS-314 Mesylate LY3295668 SP-96	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

Aurora Kinase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	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
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生物活性

製品説明

特性

An Aurora selective ATP-competitive inhibitor.

Targets

Aurora A ^[1] (Cell-free assay)	Aurora B ^[1] (Cell-free assay)	LCK ^[1] (Cell-free assay)	Src ^[1] (Cell-free assay)	MEK1 ^[1] (Cell-free assay)
110 nM	130 nM	880 nM	1.03 μM	1.79 μM

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. ^[4]
Kinase Assay	In vitro kinase assays
Kinase Assay	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 Betaplate^TM 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

参考
[1] Ditchfield C, et al. J Cell Biol. 2003, 161(2), 267-280. [2] Georgieva I, et al. Neuroendocrinology. 2010, 91(2), 121-130. [3] Teperek-Tkacz M, et al. Cell Cycle. 2010, 9(23), 4674-4687. [4] Zhang L, et al. J Obstet Gynaecol Res. 2011, 37(6), 591-600. + 展開

参考

[4] Zhang L, et al. J Obstet Gynaecol Res. 2011, 37(6), 591-600.

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

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
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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