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BMS265246

potent and selective CDK1/2 inhibitor

BMS265246

Catalog No. A8385
Size Price Stock Qty
5mg $284.00 In stock
10mg $389.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BMS265246

Biological Activity

Description BMS-265246 is a potent and selective inhibitor of CDK1 and CDK2 with IC50 values of 6 nM and 9 nM, respectively.
Targets CDK1/CyclinB CDK2/CyclinE CDK4/CyclinD      
IC50 6 nM 9 nM 230 nM      

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Chemical Properties

Cas No. 582315-72-8 SDF Download SDF
Chemical Name (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
Canonical SMILES CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F
Formula C18H17F2N3O2 M.Wt 345.34
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

Background

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.