PF 03814735

Pricing Availability Delivery Time Qty
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
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

PF 03814735 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: PF03814735 Pfizer Aurora kinase A B inhibitors inhibits antiproliferative Aurora Kinases

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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.

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