PF 03814735 (Aurora Kinases A and B, N-[2-[(1S,4R)-6-[[4-(Cyclobutylamin o)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3, 4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- acetamide)

ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5nm 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 ~20, 50 and 150nm 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.\n\nSequence:\nC23H25F3N6O2\n\nSolubility:\nDMSO (~100mM), Ethanol (~20mM)\n\nMolecular Weight:\n~474.48\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.

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SPECIFICATIONS

Catalog Number

145687

Size

10mg

Form

Supplied as a white solid.

Purity

~98% (HPLC)

References

1. Jani et al (2010) PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 9:883. PMID: 20354118. 2. 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. 3. Kollareddy et al (2012) Aurora kinase inhibitors: progress towards the clinic. Invest.New Drugs 30:2411. PMID: 22350019.