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)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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Technical Data

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.

Solubility Data

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

Preparing Stock Solutions

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.

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

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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Keywords: PF 03814735, PF 03814735 supplier, PF03814735, Pfizer, Aurora, kinase, A, B, inhibitors, inhibits, antiproliferative, Kinases, Viral, Transduction, Enhancers, 4821, Tocris Bioscience

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