ZM447439 is a potent and selective inhibitor of aurora-A and -B kinase with putative anti-tumoral activity. ZM induced apoptosis in a concentration- and time-dependent manner.

Product information

CAS Number: 331771-20-1

Molecular Weight: 513.59

Formula: C29H31N5O4

Synonym:

ZM447439

ZM 447439

Chemical Name: N-(4-((6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-yl)amino)phenyl)benzamide

Smiles: COC1=CC2=C(NC3=CC=C(C=C3)NC(=O)C3C=CC=CC=3)N=CN=C2C=C1OCCCN1CCOCC1

InChiKey: OGNYUTNQZVRGMN-UHFFFAOYSA-N

InChi: InChI=1S/C29H31N5O4/c1-36-26-18-24-25(19-27(26)38-15-5-12-34-13-16-37-17-14-34)30-20-31-28(24)32-22-8-10-23(11-9-22)33-29(35)21-6-3-2-4-7-21/h2-4,6-11,18-20H,5,12-17H2,1H3,(H,33,35)(H,30,31,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 103 mg/mL(200.54 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle. In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle. A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin.

References:

1. Teperek-Tkacz M, et al. Cell Cycle. 2010, 9(23), 4674-4687.
2. Georgieva I, et al. Neuroendocrinology. 2010, 91(2), 121-130.
3. Ditchfield C, et al. J Cell Biol. 2003, 161(2), 267-280.

Products are for research use only. Not for human use.