PF 03814735

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Cat.No. 4821 - PF 03814735 | C23H25F3N6O2 | CAS No. 942487-16-3
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)
Literature (3)

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.

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
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.

Solubility Data for PF 03814735

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 47.45 100
ethanol 9.49 20

Preparing Stock Solutions for PF 03814735

The following data is based on the product molecular weight 474.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.11 mL 10.54 mL 21.08 mL
5 mM 0.42 mL 2.11 mL 4.22 mL
10 mM 0.21 mL 1.05 mL 2.11 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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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

If you know of a relevant reference for PF 03814735, please let us know.

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.