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.

Legal Information

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

Other Notes

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

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Regulatory Review (Z)