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Merck
CN

189410

Aurora Kinase Inhibitor VI, ZM447439

The Aurora Kinase Inhibitor VI, ZM447439, also referenced under CAS 331771-20-1, controls the biological activity of Aurora Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

Aurora Kinase Inhibitor VI, ZM447439, 4-(4-(N-Benzoylamino)anilino)-6-methoxy-7-(3-(1-morpholino)propoxy)quinazoline

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关于此项目

经验公式(希尔记法):
C29H31N5O4
化学文摘社编号:
分子量:
513.59
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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)

SMILES string

O=C(C1=CC=CC=C1)NC(C=C2)=CC=C2NC3=NC=NC4=C3C=C(OC)C(OCCCN5CCOCC5)=C4

InChI key

OGNYUTNQZVRGMN-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 50 mg/mL

shipped in

ambient

Quality Level

General description

A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50 = 110 and 130 nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50 = 0.88, 1.03 and 1.79 µM for Lck, Src and MEK1, respectively, and IC50 >10 µM for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20 µM, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Gadea, B.B. and Ruderman, J.V., 2005. Mol. Biol. Cell16, 1305.
Ditchfield, C., et al. 2003. J. Cell Biol.161, 267.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Federico Gulluni et al.
Science (New York, N.Y.), 374(6573), eabk0410-eabk0410 (2021-12-10)
Cytokinetic membrane abscission is a spatially and temporally regulated process that requires ESCRT (endosomal sorting complexes required for transport)–dependent control of membrane remodeling at the midbody, a subcellular organelle that defines the cleavage site. Alteration of ESCRT function can lead
Onur Sen et al.
Developmental cell, 56(22), 3082-3099 (2021-11-11)
Chromosome mis-segregation during mitosis leads to aneuploidy, which is a hallmark of cancer and linked to cancer genome evolution. Errors can manifest as "lagging chromosomes" in anaphase, although their mechanistic origins and likelihood of correction are incompletely understood. Here, we

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