Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

PubChem22455 4-[[5-amino-1-(2,6- difluorophenyl)carbonyl...

Synonyms: Kinome_3748, S1249_Selleck, CHEMBL191003, cc-474, SureCN1060773, ...

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High impact information on JNJ-7706621

The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases [1].
In human cancer cells, treatment with JNJ-7706621 inhibited cell growth independent of p53, retinoblastoma, or P-glycoprotein status; activated apoptosis; and reduced colony formation [1].
These results show the therapeutic potential of this novel cell cycle inhibitor and support clinical evaluation of JNJ-7706621 [1].
Flow cytometric analysis of DNA content showed that JNJ-7706621 delayed progression through G1 and arrested the cell cycle at the G2-M phase [1].
ABCG2 is likely to limit the bioavailability of JNJ-7706621 because oral administration of JNJ-7706621 to Bcrp (the murine homologue of ABCG2) knockout mice resulted in an increase in the plasma concentration of JNJ-7706621 compared with wild-type mice [2].

Anatomical context of JNJ-7706621

To determine the putative mechanisms of resistance to JNJ-7706621 that might be encountered in the clinic, the human epithelial cervical carcinoma cell line (HeLa) was exposed to incrementally increasing concentrations of JNJ-7706621 [2].

Associations of JNJ-7706621 with other chemical compounds

One such molecule, JNJ-7706621, is a broad-spectrum inhibitor of the cyclin-dependent kinases and Aurora kinases that mediate G(2)-M arrest and inhibits tumor growth in xenograft models [2].

References

The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Emanuel, S., Rugg, C.A., Gruninger, R.H., Lin, R., Fuentes-Pesquera, A., Connolly, P.J., Wetter, S.K., Hollister, B., Kruger, W.W., Napier, C., Jolliffe, L., Middleton, S.A. Cancer Res. (2005) [Pubmed]
Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Seamon, J.A., Rugg, C.A., Emanuel, S., Calcagno, A.M., Ambudkar, S.V., Middleton, S.A., Butler, J., Borowski, V., Greenberger, L.M. Mol. Cancer Ther. (2006) [Pubmed]

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