Translational Bioscience offers an experienced perspective in vitro cellular studies. Whether preliminary efficacy studies based on viability or more detailed assessment of the MOA of your molecule, we are here to help.
Investigation of a Cytostatic Molecule
We developed a robust model for studying a potentially novel CDK4/6 inhibitor. For these studies, Palbociclib an FDA approved potent and highly selective CDK4/6 inhibitor, was used as a control. This small molecule compound can inhibit CDK4/6 in vitro, resulting in loss of Rb (retinoblastoma) phosphorylation and thus, functions as a cytostatic agent. It induces G1 arrest and cellular senescence (to be backed up by senescence data) in vitro and inhibits growth of tumor xenografts in vivo 1. The data below shows anti-proliferative effects of Palbociclib in an ER+ cell line using BrdU incorporation as a readout.
- Vijayaraghavan, Smruthi et al. “CDK4/6 and Autophagy Inhibitors Synergistically Induce Senescence in Rb Positive Cytoplasmic Cyclin E Negative Cancers.” Nature Communications 8 (2017): 15916. PMC. Web. 3 Oct. 2017.
- Richard S Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J Cohen, Amrita J Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los, Dennis J Slamon, Breast Cancer Research, 11: R77, 2009