ZM-447439

Name: ZM-447439
Brand: MedChemExpress
SKU: HY-10128
Rating: 5.0 (7 reviews)

製品番号: HY-10128 純度: 98.94%: Data Sheet SDS COA 取扱説明書
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ZM-447439 is an aurora kinase inhibitor with IC₅₀s of 110 and 130 nM for aurora A and B, respectively.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

ZM-447439 構造式

CAS 番号 : 331771-20-1

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 68	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 68	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$96	在庫あり	Estimated Time of Arrival: December 31
25 mg	$180	在庫あり	Estimated Time of Arrival: December 31
50 mg	$286	在庫あり	Estimated Time of Arrival: December 31
100 mg	$495	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of ZM-447439:

ZM-447439 (Standard) お問い合わせ

顧客検証

Aurora Kinase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Aurora Kinase Aurora A Aurora B Aurora C

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

ZM-447439 is an aurora kinase inhibitor with IC₅₀s of 110 and 130 nM for aurora A and B, respectively.

IC₅₀ & Target^[1]

Aurora A

110 nM (IC₅₀)

Aurora B

130 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.3 3 Compound: ZM447439	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	[PMID: 25270403]
A549	IC₅₀	3.3 3 Compound: ZM447439	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	[PMID: 25270403]
HepG2	IC₅₀	1.4 3 Compound: ZM447439	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	[PMID: 28279846]
HepG2	IC₅₀	1.4 3 Compound: ZM447439	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	[PMID: 28279846]
HT-29	IC₅₀	2.2 3 Compound: ZM447439	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	[PMID: 25270403]
HT-29	IC₅₀	2.2 3 Compound: ZM447439	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	[PMID: 25270403]
K562	IC₅₀	> 100 3 Compound: ZM447439	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	[PMID: 25270403]
K562	IC₅₀	>100 3 Compound: ZM447439	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	[PMID: 25270403]
A549	IC₅₀	3.3 3 Compound: ZM447439	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	[PMID: 25270403]
LoVo	IC₅₀	1.9 3 Compound: ZM447439	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	[PMID: 25270403]
LoVo	IC₅₀	1.9 3 Compound: ZM447439	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	[PMID: 25270403]
NCI-H661	IC₅₀	2.9 3 Compound: ZM447439	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	[PMID: 25270403]
MCF7	IC₅₀	198 1 Compound: 2	Antiproliferative activity against MCF7 cell line Antiproliferative activity against MCF7 cell line	[PMID: 16337122]
NCI-H661	IC₅₀	2.9 3 Compound: ZM447439	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	[PMID: 25270403]
U-937	IC₅₀	> 100 3 Compound: ZM447439	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	[PMID: 25270403]
U-937	IC₅₀	>100 3 Compound: ZM447439	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	[PMID: 25270403]
HT-29	IC₅₀	2.2 3 Compound: ZM447439	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	[PMID: 25270403]
HepG2	IC₅₀	1.4 3 Compound: ZM447439	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	[PMID: 28279846]
K562	IC₅₀	> 100 3 Compound: ZM447439	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	[PMID: 25270403]
LoVo	IC₅₀	1.9 3 Compound: ZM447439	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	[PMID: 25270403]
MCF7	IC₅₀	198 1 Compound: 2	Antiproliferative activity against MCF7 cell line Antiproliferative activity against MCF7 cell line	[PMID: 16337122]
NCI-H661	IC₅₀	2.9 3 Compound: ZM447439	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	[PMID: 25270403]
U-937	IC₅₀	> 100 3 Compound: ZM447439	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	[PMID: 25270403]

体外実験

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.

分子量

513.59

分子式

C₂₉H₃₁N₅O₄

CAS 番号

331771-20-1

Appearance

Solid

Color

White to gray

SMILES

O=C(NC1=CC=C(NC2=C(C(C=C3OCCCN4CCOCC4)=NC=N2)C=C3OC)C=C1)C5=CC=CC=C5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9471 mL	9.7354 mL	19.4708 mL
5 mM	0.3894 mL	1.9471 mL	3.8942 mL
10 mM	0.1947 mL	0.9735 mL	1.9471 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.19%

Select Batch:

データシート (274 KB) SDS (393 KB)

COA (246 KB) LCMS (108 KB)

取扱説明書 (2659 KB)

参考文献

[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]

キナーゼ実験 ^[1]	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) はこれらの方法の精度を確認していません。こちらは参照専用です。
細胞実験 ^[1]	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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZM-447439331771-20-1ZM447439ZM 447439Aurora KinaseApoptosisInhibitorinhibitorinhibit

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参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ZM-447439 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Other Forms of ZM-447439:

ZM-447439 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Aurora Kinase アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

ZM-447439 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ZM-447439 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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