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Description: Aurora kinase A and B inhibitor
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
Purity: ≥98% (HPLC)
Biological Activity for PF 03814735
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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 03814735
PF 03814735 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 03814735
| M. Wt | 474.48 |
| Formula | C23H25F3N6O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 942487-16-3 |
| PubChem ID | 51346455 |
| InChI Key | RYYNGWLOYLRZLK-RBUKOAKNSA-N |
| Smiles | [H][C@@]3(N5C(CNC(C)=O)=O)CC[C@@]5([H])C(C3=C4)=CC=C4NC1=NC(NC2CCC2)=C(C(F)(F)F)C=N1 |
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.
Product Datasheets for PF 03814735
References for PF 03814735
References are publications that support the biological activity of the product.
Jani et al (2010) PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 9 883 PMID: 20354118
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
Maddelena et al (2018) High-throughput screening identifies kinase inhibitors that increase dual adeno-sssociated viral vector transduction in vitro and in mouse retina. Hum.Gene.Ther. 29 886 PMID: 29641320
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Cell Cycle and DNA Damage Research Product Guide
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