PF 03814735

Biological Activity

PF 03814735 is an ATP-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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy.
   Jani et al.
   Mol.Cancer Ther., 2010;9:883
2. 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
3. Aurora kinase inhibitors: progress towards the clinic.
   Kollareddy et al.
   Invest.New Drugs, 2012;30:2411
4. High-throughput screening identifies kinase inhibitors that increase dual adeno-sssociated viral vector transduction in vitro and in mouse retina.
   Maddelena et al.
   Hum.Gene.Ther., 2018;29:886

Product Datasheets