Chemical Name: N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
Biological ActivityATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5 nM for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are approximately 20, 50 and 150 nM respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Orally available.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy.
Jani et al.
Mol.Cancer Ther., 2010;9:883
An integrated genomic approach to identify predictive biomarkers of response to the Aurora kinase inhibitor PF-03814735.
Hook et al.
Mol.Cancer Ther., 2012;11:710
Aurora kinase inhibitors: progress towards the clinic.
Kollareddy et al.
Invest.New Drugs, 2012;30:2411
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