PF 03814735

Name: PF 03814735
Brand: Tocris Bioscience
SKU: 4821

Tocris Bioscience, part of Bio-Techne | Catalog # 4821

COA / SDS

Aurora kinase A and B inhibitor

Discontinued Product

4821 has been discontinued. View all Aurora Kinase Inhibitors products.

Key Product Details

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)
Molecular Weight:	474.48

View Full Technical Details for PF 03814735

Technical Data
Citations

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.

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References for PF 03814735

References are publications that support the biological activity of the product.

Maddelena High-throughput screening identifies kinase inhibitors that increase dual adeno-sssociated viral vector transduction in vitro and in mouse retina. Hum.Gene.Ther. 2018 PMID: 29641320
Hook An integrated genomic approach to identify predictive biomarkers of response to the Aurora kinase inhibitor PF-03814735. Mol.Cancer Ther. 2012 PMID: 22222631
Kollareddy Aurora kinase inhibitors: progress towards the clinic. Invest.New Drugs 2012 PMID: 22350019
Jani PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 2010 PMID: 20354118