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PF 03814735
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C23H25F3N6O2
- MW: 474.48
Description
PF 03814735 is a potent, orally bioavailable, ATP-competitive Aurora A and Aurora B kinase inhibitor with reported IC50 values of 0.8 nM and 5 nM, respectively. It also inhibits Flt1, FAK and TrkA in reported profiling.
Aurora kinases regulate mitotic entry, chromosome segregation and cytokinesis. PF 03814735 is useful for studying pan-Aurora pathway inhibition, mitotic failure and antineoplastic mechanisms in cell-cycle-dependent tumor models.
Key Features
- Potent Aurora A/B kinase inhibitor
- Reported IC50: 0.8 nM (Aurora A) and 5 nM (Aurora B)
- Orally bioavailable and ATP-competitive pharmacology
- Additional activity reported against Flt1, FAK and TrkA
Applications
- Aurora kinase assays
- Mitosis and cytokinesis studies
- Cancer cell-cycle research
- Kinase inhibitor selectivity profiling
More Information
| Parent CAS No. | 942487-16-3 |
|---|---|
| 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 |
| extra_info | . |
| SMILES | C1(NC2CCC2)C(C(F)(F)F)=CN=C(N=1)NC1=CC=C2C3CCC([N@@]3C(=O)CNC(=O)C)C2=C1 |&1:24,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C23H25F3N6O2/c1-12(33)27-11-20(34)32-18-7-8-19(32)16-9-14(5-6-15(16)18)30-22-28-10-17(23(24,25)26)21(31-22)29-13-3-2-4-13/h5-6,9-10,13,18-19H,2-4,7-8,11H2,1H3,(H,27,33)(H2,28,29,30,31)/t18-,19+/m0/s1 |
| InChiKey | RYYNGWLOYLRZLK-RBUKOAKNSA-N |
| CID | 51346455 |
| Short Description | Aurora inhibitor |
References
- JP Jani et al. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol. Cancer Ther. 2010, 9(4), 883-894.
- P Schöffski et al. Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours. Eur. J. Cancer. 2011, 47(15), 2256-2264.
- KE Hook et al. An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. Mol. Cancer Ther. 2012, 11(3), 710-719.
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