ZM-447439 CAS: 331771-20-1
MF: C29H31N5O4
MW: 513.6
A selective inhibitor of ARK-1, ARK-2, and ARK-3.

ZM-447439 (CAS 331771-20-1)

ZM-447439 | CAS 331771-20-1 is rated 5.0 out of 5 by 1.
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Alternate Names: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
Application: ZM-447439 is a selective inhibitor of ARK-1, ARK-2, and ARK-3
CAS Number: 331771-20-1
Purity: ≥99%
Molecular Weight: 513.6
Molecular Formula: C29H31N5O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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ZM-447439 is a selective inhibitor of aurora kinases ARK-1 (A) (IC50=1000 nM, Ki=100nM), ARK-2 (B) (IC50= 50 nM, Ki= 0.36 nM) and ARK-3 (C), that can induce growth arrest, inhibit histone H3 phosphorylation and effectively activate apoptosis. The compound specifically interacts at the ATP-binding site and at the adjacent cleft, found only in aurora kinases. In the presence of Z-M447439, chromosome alignment, segregation, and cytokinesis during mitosis are unsuccessful. Studies show that ZM-447439 can override the spindle assembly checkpoint and accelerate meiosis I in mouse oocytes.


References

1. Ditchfield, C., et al. 2003. J. Cell Biol. 161: 267-280. PMID: 12719470
2. Long, Z.J., et al. 2008. Cell Cycle. 7: 1473-1479. PMID: 18418083
3. Walsby, E., et al. 2008. Haematologica. 93: 662-669. PMID: 18367484
4. Georgieva, I., et al. 2010. Neuroendocrinology. 91: 121-130. PMID: 19923785
5. Lane, S.I., et al. 2010. Reproduction. 140: 521-530. PMID: 20660090

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), methanol, water (<1 mg/ml) at 25° C, ethanol (48 mg/ml) at 25° C, DMF (~20 mg/ml), and DMSO:PBS (1:1, pH 7.2) (~0.5 mg/ml).
Storage :
Store at room temperature
Melting Point :
117-120° C
Boiling Point :
639.67° C at 760 mmHg (Predicted)
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
Aurora A kinase: IC50 = 1 µM; Aurora B kinase: IC50 = 50 nM; Aurora C kinase: IC50 = 250 nM; cdk1: IC50 > 10 µM; PLK1: IC50 > 10 µM; MCF7: IC50 = 198 nM (human)
Ki Data :
ARK-1 (A): Ki= 100 nM; ARK-2 (B) : Ki= 0.36 nM
pK Values :
pKa: 13.01 (Predicted), pKb: 6.99 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :
MFCD08703125
SMILES :
COC1=C(OCCCN2CCOCC2)C=C2N=CN=C(NC3=CC=C(NC(=O)C4=CC=CC=C4)C=C3)C2=C1

Download SDS (MSDS)

Certificate of Analysis

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ZM-447439 (CAS 331771-20-1)  Product Citations

See how others have used ZM-447439 (CAS 331771-20-1). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 33397691  Kawashima, AT.|Wong, C.|Lordén, G.|King, CC.|Lara-Gonzalez, P.|Desai, A.|Gingras, AC.|Newton, AC.| et al. 2021. Mol Cell Biol.

PMID: # 27249336  Qi, D. et al. 2016. Cell Cycle. 15: 2009-18.

PMID: # 27656108  Luján, P. et al. 2016. J. Cell. Sci. 129: 4130-4142.

PMID: # 22890557  Lan, R. et al. 2012. Lab. Invest. 92: 1503-14.

PMID: # 19150808  Liu, D. et al. 2009. Science. 323: 1350-1353.

PMID: # 18367484  Walsby, E. et al. 2008. Haematologica. 93: 662-669.

PMID: # 17394948  Kim, KW. et al. 2007. Int. J. Radiat. Oncol. Biol. Phys. 67: 1519-1525.

PMID: # 17567953  Zhang, X. et al. 2007. Mol. Biol. Cell. 18: 3264-3276.

PMID: # 16046481  Morrow, CJ. et al. 2005. J. Cell. Sci. 118: 3639-3652.

PMID: # 26011858  Elife. 4: e06547.

Citations 1 to 10 of 14 total
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Rated 5 out of 5 by from Liu et al Liu et al. (PubMedID 19150808) used ZM-447439, a reversible Aurora B kinase inhibitor, to prevent the phosphorylation of kinetochore substrates necessary for adequate cell division. -SCBT Publication Review
Date published: 2015-05-03
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