Related Experiment Video
Updated: May 22, 2026

Pooled shRNA Screen for Reactivation of MeCP2 on the Inactive X Chromosome
Published on: March 2, 2018
Discovery of XL413, a potent and selective CDC7 inhibitor
Elena S Koltun1, Amy Lew Tsuhako, David S Brown
1Exelixis, Department of Drug Discovery, South San Francisco, CA 94080, USA. elena@numerate.com
Abstract:
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.
Related Concept Videos
Inhibition of Cdk Activity
Inhibition of CDK Activity
