ZM 447439

Bezeichnung:ZM 447439

CAS-Nr331771-20-1

Englisch Name:ZM 447439

CBNumberCB8849467

SummenformelC29H31N5O4

Molgewicht513.59

MOL-Datei331771-20-1.mol

ZM 447439 physikalisch-chemischer Eigenschaften

Schmelzpunkt	117-120°C
Siedepunkt	639.7±55.0 °C(Predicted)
Dichte	1.282±0.06 g/cm3(Predicted)
storage temp.	Desiccate at RT
Löslichkeit	Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml).
Aggregatzustand	White solid
pka	13.01±0.70(Predicted)
Farbe	White
Stabilität	Stable for 1 year from date of purchase? as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Gefahreninformationscode (GHS)

ZM 447439 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
The Aurora kinases have important roles in regulating mitosis and cytokinesis, with Aurora B involved in centromere function as part of the Chromosomal Passenger Complex, with survivin, INCENP, and borealin. ZM 447439 is a selective inhibitor of Aurora B kinase (IC₅₀ = 50 nM), less potently inhibiting Aurora C and A (IC₅₀ = 250 and 1,000 nM, respectively). It has no effect on several other kinases, including Cdk1, Cdk2, Cdk4, Plk1, CHK1, KDR2, and FAK (IC₅₀ > 10 μM). ZM 447439 has been used to study the role of Aurora B in molecular events associated with mitosis and cytokinesis. Moreover, ZM 447439 selectively inhibits proliferating cells rather than non-dividing cells, suggesting its potential in cancer therapy.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
It is a potent and selective inhibitor of Aurora B kinase. Cells treated with ZM-447439 progress through interphase, enter mitosis and assemble bipolar spindles but chromosome alignment, segregation and cytokinesis all fail. It induces apoptosos in Hep2 cancer cells and in acute myeloid leukemia cell lines but its propensity to induce polyploidy does not inevitably result in apoptosis.
Definition
ChEBI: ZM447439 is a member of the class of quinazolines that is quinazoline which is substituted at positions 4, 6 and 7 by a (4-benzamidophenyl)nitrilo group, methoxy group and a 3-(morpholin-4-yl)propoxy group, respectively. It is an ATP-competitive inhibitor of Aurora A and Aurora B kinases with IC50 of 110 nM and 130 nM, respectively. It has a role as an Aurora kinase inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of benzamides, a member of quinazolines, an aromatic ether, a member of morpholines, a polyether, a secondary amino compound and a tertiary amino compound.
Lager
room temperature (desiccate)
Einzelnachweise
1) Ditchfield et al (2003) Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores; J.Cell Biol. 161 267 2) Girdler et al. (2006) Validating Aurora B as an anti-cancer drug target; J. Cell Sci. 119 3664

ZM 447439 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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