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ZM 447439
| Product Name | ZM 447439 |
| Price: | Inquiry |
| Catalog No.: | CN00418 |
| CAS No.: | 331771-20-1 |
| Molecular Formula: | C29H31N5O4 |
| Molecular Weight: | 513.59 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | COc1cc2c(ncnc2cc1OCCCN1CCOCC1)Nc1ccc(cc1)NC(=O)c1ccccc1 |
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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. |
| Target | 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]. |
| Cell Assay | 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]. |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 639.7±55.0 °C at 760 mmHg |
| Flash Point | 340.7±31.5 °C |
| Exact Mass | 513.237610 |
| PSA | 97.84000 |
| LogP | 2.66 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Storage condition | Desiccate at RT |