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. Also enhances adeno-associated virus transduction of retina cells in vitro and in vivo. Orally available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
High-throughput screening identifies kinase inhibitors that increase dual adeno-sssociated viral vector transduction in vitro and in mouse retina.
Maddelena et al.
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