|potent and selective CDK1/2 inhibitor|
Sample solution is provided at 25 µL, 10mM.
|Description||BMS-265246 is a potent and selective inhibitor of CDK1 and CDK2 with IC50 values of 6 nM and 9 nM, respectively.|
|IC50||6 nM||9 nM||230 nM|
|Cas No.||582315-72-8||SDF||Download SDF|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
|Shipping Condition:||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
BMS265246 is a potent and selective Cdk1/Cdk2 inhibitor for Cdk1/cyclin-B (IC50 = 6 nM) and Cdk2/cyclin-E (IC50 = 9 nM). BMS265246 inhibits the activity of Cdk4/cycD (IC50 = 0.23 μM) and prevents A2780 Cytox with IC50 of 0.76 μM. BMS265246 when bound to Cdk2, shows the inhibitor resides within the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS265246 represents the most potent Cdk/Cdk2 selective analogue from this chemotype. A recent study shows that BMS-265246 inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of BMS-265246, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity.