PF 03814735

Cat. No. 4821

PF 03814735 C23H25F3N6O2 [942487-16-3]

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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 Activity

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. Orally available.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
474.48
Formula:
C23H25F3N6O2
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
942487-16-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Hook et al (2012) An integrated genomic approach to identify predictive biomarkers of response to the Aurora kinase inhibitor PF-03814735. Mol.Cancer Ther. 11 710. PMID: 22222631.

Kollareddy et al (2012) Aurora kinase inhibitors: progress towards the clinic. Invest.New Drugs 30 2411. PMID: 22350019.

Jani et al (2010) PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 9 883. PMID: 20354118.

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Keywords: PF 03814735, supplier, PF03814735, Pfizer, Aurora, kinase, A, B, inhibitors, inhibits, antiproliferative, Tocris Bioscience, Aurora Kinase Inhibitor products

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