The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma

CCT245737 is the first orally active, clinical development candidate CHK1 inhibitor to be described. The IC(50) was 1.4nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently inhibited cellular CHK1 activity (IC(50) 30-220nM) and enhanced gemcitabi...

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Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:Oncotarget
Prif Awduron: Walton, Mike I., Eve, Paul D., Hayes, Angela, Henley, Alan T., Valenti, Melanie R., De Haven Brandon, Alexis K., Box, Gary, Boxall, Kathy J., Tall, Matthew, Swales, Karen, Matthews, Thomas P., McHardy, Tatiana, Lainchbury, Michael, Osborne, James, Hunter, Jill E., Perkins, Neil D., Aherne, G. Wynne, Reader, John C., Raynaud, Florence I., Eccles, Suzanne A., Collins, Ian, Garrett, Michelle D.
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: Impact Journals LLC 2015
Pynciau:
Research Paper
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC4823038/
https://ncbi.nlm.nih.gov/pubmed/26295308
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.18632/oncotarget.4919
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