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
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
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
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- UPC:
- 51343601
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 189410-5MG
- CAS:
- 331771-20-1
- Temperature Control Device:
- Yes
