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ZM447439

Cat. No. M1877

ZM447439 Structure

Synonym: ZM-447439

Size Price Availability Quantity
10mg USD 90 In stock
25mg USD 180 In stock
50mg USD 280 In stock
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Quality Control
Biological Activity

ZM447439 is an Aurora kinase B inhibitor, suppresses the growth of cervical cancer SiHa cells and enhances the chemosensitivity to cisplatin. Aurora family kinases play roles in several mitotic processes, including the G2/M transition, mitotic spindle organization, chromosome segregation, and cytokinesis. ZM447439 has dramatic effects on chromosome morphology and spindle dynamics. ZM-447439 can reduce the number of SiHa cells, increase the volume of cells and lead to apoptosis. The growth of SiHa cells treated with ZM447439 was inhibited in dose- and time-dependent manners. ZM447439 significantly inhibited the expression of Aurora-B and H3-P protein (P < 0.05). ZM-447439 selectively over a range of other kinases such as Cdk1 and PLK1 (up to 10mM). Additionally, aurora kinase inhibition by ZM447439 potently induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation.

Protocol
Cell Experiment
Cell lines MCF7 cells
Preparation method Cell cycle analysis and cloning assays. DNA content and mitotic index measurements and synchronization of TA-HeLa cells at G1/S using a double thymidine block were done as described previously (Taylor and McKeon, 1997). To determine cloning efficiency, MCF7 cells were plated in phenol red free DME plus 5% stripped serum (HyClone), and were then treated with or without the anti-estrogen ICI 182780 at 1 μM for 48 h. ZM447439 was then added at the indicated concentrations for 72 h. The cells were harvested, washed, and ∼400 cells plated in each well of a 6-well plate in complete media without ZM447439. After 10 d, the colonies were fixed, stained with crystal violet, and counted. The cloning efficiency represents the number of colonies on ZM447439-treated plates compared with DMSO-treated controls.
Concentrations 0~5 μM
Incubation time 72 h
Animal Experiment
Animal models MOLM13 cells in murine xenograft model
Formulation 3 M Tris, pH 9.0, at a concentration of 2.5 mg/mL
Dosages 5 mg/kg 4 times a week for 2 weeks
Administration intraperitoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 513.59
Formula C29H31N5O4
CAS Number 331771-20-1
Purity 98.34%
Solubility DMSO 50 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Concordia University (2015). Figure 9. ZM447439 (Abmole Bioscience)
Method Inhibit Aurora B kinase
Cell Lines MDCK cell lines
Concentrations 1 μM
Incubation Time 20-­‐40 min
Results Upon treating MDCK cells with an 35 Aurora B inhibitor, ZM447439, we found that the number asymmetrically ingressing cells was not statistically changed in comparison to control cells
Rating
References

ZM447439, a novel promising aurora kinase inhibitor, provokes antiproliferative and proapoptotic effects alone and in combination with bio- and chemotherapeutic agents in gastroenteropancreatic neuroendocrine tumor cell lines.
Georgieva I, et al. Neuroendocrinology. 2010;91(2):121-30. PMID: 19923785.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ZM447439, ZM-447439 supplier, Aurora Kinase, inhibitors

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