Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7
Jason Marineau, Kristin B. Hamman, Shanhu Hu, Sydney Alnemy, Janessa Mihalich, A. Kabro, Kenneth Matthew Whitmore, Dana K. Winter, Stéphanie Roy, Stéphane Ciblat, Nan Rosemary Ke, Anneli Savinainen, Ashraf Wilsily, G. Malojcic, Robert Zahler, Darby Schmidt, Michael J. Bradley, Nigel J. Waters, Claudio Chuaqui
Abstract
displays potent inhibition of CDK7 in cells and demonstrates strong efficacy in mouse xenograft models when dosed as low as 2 mg/kg.
Topics & Concepts
ChemistryCyclin-dependent kinase 7PotencyPharmacophorePharmacologyBiochemistryComputational biologyCellCell cycleIn vitroCyclin-dependent kinase 2BiologyMedicineCancer-related Molecular PathwaysCancer therapeutics and mechanismsLung Cancer Research Studies