ZM-447439 , ≥98% , 331771-20-1

Synonym(s):
4-(4-(N-Benzoylamino)anilino)-6-methoxy-7-(3-(1-morpholino)propoxy)quinazoline;Aurora Kinase Inhibitor VI, ZM447439 - CAS 331771-20-1 - Calbiochem

CAS NO.：331771-20-1

Empirical Formula: C29H31N5O4

Molecular Weight: 513.59

MDL number: MFCD08703125

PRODUCT Properties

• Melting point: 117-120°C
• Boiling point: 639.7±55.0 °C(Predicted)
• Density: 1.282±0.06 g/cm3(Predicted)
• storage temp.: Desiccate at RT
• solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml).
• form: White solid
• pka: 13.01±0.70(Predicted)
• color: White
• Stability: 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.

Description and Uses

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.

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.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319
• Precautionary statements: P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313