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

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 IC50 was 1.4nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently inhibited cellular CHK1 activity (IC50 30-220nM) and enhanced gemcitabine a...

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Bibliographic Details
Main Authors: 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.
Format: Online
Language:English
Published: Impact Journals LLC 2015
Online Access:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4823038/

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4823038/

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