1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Aurora Kinase Apoptosis
  3. ZM-447439

ZM-447439 

Cat. No.: HY-10128 Purity: 98.70%
COA Handling Instructions

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

For research use only. We do not sell to patients.

ZM-447439 Chemical Structure

ZM-447439 Chemical Structure

CAS No. : 331771-20-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 62 In-stock
Solution
10 mM * 1 mL in DMSO USD 62 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 286 In-stock
100 mg USD 495 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

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)

In Vitro

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.

Molecular Weight

513.59

Formula

C29H31N5O4

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (48.68 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.19%

References
Kinase Assay
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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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.

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Product Name:
ZM-447439
Cat. No.:
HY-10128
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