BMS-265246

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency: 

IC50

6 nM

Potency assay: 

CDK2 IC50 = 9 nM CDK4 IC50 = 230 nM

Structure-activity relationship: 

The 2,6-difluorophenyl substitution was critical for potent inhibitory activity.

In cell validation

On target activity in cells

Potency assay (cells): 

In high-content imaging experiments, BMS-265246 led to G2-arrest phenotypes

Toxicity

Cytoxicity assay: 

Yes

Notes on cytotoxicity: 

BMS-265246 is cytotoxic at 0.76 uM in A2780 cells.