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Purity: ≥98%
ZM 447439 (ZM-447439) is a novel, potent, selective and ATP-competitive inhibitor of Aurora A and Aurora B with potential antitumor activity. It inhibits Aurora A and Aurora B with IC50s of 110 nM and 130 nM, respectively. It shows 8-fold higher selectivity for Aurora A/B over MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. Being specifically for Aurora kinases, ZM 447439 barely inhibits the majority of other protein kinases (IC50 > 10 μM), such as CDK1/2/4, IKK1/2, PLK1, CHK1, cFLT2, KDR2, FAK and Zap-70, except for MEK1, SRC and LCK (IC50 values of 1.79 μM, 1.03 and 0.88 μM respectively.
| ln Vitro |
ZM-447439-treated cells undergo interphase, properly enter mitosis, and form bipolar spindles. On the other hand, cytokinesis, segregation, and chromosomal alignment all fail. ZM-447439 suppresses the phosphorylation of histone H3 during mitosis and limits cell division. Chromosome alignment and segregation are inhibited by ZM-447439. Function of spindle checkpoint is compromised by ZM-447439. Similar to cells with genetically inhibited Aurora-B, these ZM-treated G2/M-arrested cells accumulate 4N/8N DNA and produce multipolar spindles. The treatment with ZM-447439 causes cell death. The reduction in Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9 is potently correlated with ZM-447439 suppression of Aurora kinase[2].
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| ln Vivo |
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| References |
[1]. Ditchfield C, et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol. 2003 Apr 28;161(2):267-80.
[2]. Long ZJ, et al. ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensionalculture. Cell Cycle. 2008 May 15;7(10):1473-9 |
| Molecular Formula |
C29H31N5O4
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| Molecular Weight |
513.59
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| CAS # |
331771-20-1
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| Related CAS # |
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| SMILES |
O=C(NC1=CC=C(NC2=C3C=C(OC)C(OCCCN4CCOCC4)=CC3=NC=N2)C=C1)C5=CC=CC=C5
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| InChi Key |
OGNYUTNQZVRGMN-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-(4-((6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-yl)amino)phenyl)benzamide
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| Synonyms |
ZM-447439; ZM 447439; ZM447439.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL | |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | |
| 10 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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