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Cat. No. Name Size Price Add Cart
KI0397ZM-4474395 mg$112
ZM-44743910 mg$176
ZM-44743925 mg$432
ZM-44743950 mg$752

Chemical Characteristic

Product NameZM-447439
CAS No.331771-20-1
Molecular Weight 513.59
FormulaC29H31N5O4
Chemical NameN-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
SmilesC(=O)(c1ccccc1)Nc1ccc(cc1)Nc1ncnc2c1cc(c(c2)OCCCN1CCOCC1)OC
Chemical Structure

Biological activities

ZM-447439 is an Auroa selective ATP-competitive inhibitor that interferes with the spindle integrity checkpoint and chromosome segregation.[1] ZM-447439 inhibits aurora kinase A and aurora kinase B with IC50s of 1 μM and 50 nM, respectively.[2] ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinma cells. Suppression of Aurora kinase by ZM-447439 results in multipolar spindle structures, accumulation of cells with 4N/8N DNA content and subsequent apoptotic cell death in both dose-dependent and time-dependent manners. ZM-447439 inhibits tumor mass growth and causes apoptotic cell death in 3D carcinoma cell culture. Also, inactivation of aurora kinase by ZM-447439 reduces phosphorylation of Akt and GSK3α/β in Hep2 cells.[1] ZM-447439 has been shown to efficiently disrupt aurora B function, leading to defective cytokinesis in several types of tumor cells, including A549 reduced non-small cell lung carcinomas (NSCLC) cells. 1 μM ZM-447439 dramatically reduces the growth of NSCLC cell lines H460 and H322 after 72 hours incubation compared with untreated control samples. [3] ZM-447439 binds both the ATP-binding site and the adjacent cleft, with ZM-447439 having specificity for aurora kinases. Besides, ZM-447439 induces growth arrest and the accumulation of hyperploid cells in acute myeloid leukemia cell lines and primary acute myeloid leukemia cultures. In cell lines, the effect of 48 hours of treatment with ZM-447439 is a significant decrease in phosphorylation to 60% of the control level. In primary samples from AML patients, 0.1 µM ZM-447439 inhibits phosphorylation of histone H3 to 58% of the control level by 48 hours. Meanwhile, ZM-447439 has an effect on resulting in accumulation of cells with 4N DNA content in a variety of human cell lines (A549, MCF-7, DLD-1, HeLa and U2OS). [2]

Protocols

ZM-447439 is stored at −20 °C at 10 mM in DMSO and is diluted with culture medium immediately before use. [1]

References

[1] Long ZJ, et al. ZM-447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensional culture. Cell Cycle. 2008, 7(10): 1473-1479.
[2] Elisabeth W, et al. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica. 2008, 93(5): 662-669.
[3] Barbara V, et al. Frequent overexpression of aurora B kinase, a novel drug target, in non-small cell lung carcinoma patients. Mol Cancer Ther. 2006, 5: 2905-2913.

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