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BMS-265246

Catalog No. T2679   CAS 582315-72-8
Synonyms: BMS265246

BMS-265246 is a potent and selective CDK1/2 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
BMS-265246 Chemical Structure
BMS-265246, CAS 582315-72-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
5 mg In stock $ 113.00
10 mg In stock $ 197.00
25 mg In stock $ 389.00
50 mg In stock $ 589.00
100 mg In stock $ 843.00
500 mg In stock $ 1,730.00
1 mL * 10 mM (in DMSO) In stock $ 125.00
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Purity: 99.55%
Purity: 98.77%
Purity: 98.33%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-265246 is a potent and selective CDK1/2 inhibitor.
Targets&IC50 CDK4-CyclinD:230 nM, CDK2-CyclinE:9 nM, CDK1-CyclinB:6 nM
Kinase Assay CDK1/Cyclin B1 Kinase Assay: Kinase reactions consists of 100 ng of baculovirus expressed GST-CDK1/cyclin B1 complex, 1 μg histone H1, 0.2 μCi 33P γ-ATP, 25 μM ATP in 50 μL of kinase buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT). Reactions are incubated for 45 min at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 15%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96 well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of kinase activity (IC50). BMS265246 is dissolved at 10 mM in DMSO and evaluated at six concentrations, each in triplicate. The final concentration of DMSO in the assay equals 2%. IC50 values are derived by nonlinear regression analysis and have a coefficient of variance (SD/mean, n = 6) = 16%.
Cell Research HCT-116 cells are plated onto 96-well dishes. For each well, the cell density is calculated by counting the number of objects (cells) per field of view, and averaging across all fields for a given well. For a treatment compound, cell density is converted to a percentage relative to the plate-averaged cell density from DMSO treatment (i.e., 100% corresponds to the average cell density for DMSO treatment). Logistic regression curve fits are done using TIBCO Spotfire, and the concentration at which the curve crosses 50% is reported as the EC50 of BMS-265246.(Only for Reference)
Synonyms BMS265246
Molecular Weight 345.34
Formula C18H17F2N3O2
CAS No. 582315-72-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (46.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Misra RN, et al. Bioorg Med Chem Lett. 2003, 13(14), 2405-2408. 2. Sutherland JJ, et al. Mol Cancer Ther. 2011, 10(2), 242-254.

TargetMolCitations

1. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library NO PAINS Compound Library Cell Cycle Compound Library Anti-Aging Compound Library Anti-Prostate Cancer Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

BMS-265246 582315-72-8 Cell Cycle/Checkpoint CDK Pyrazolopyridine Inhibitor iTreg cell A2780 Angiotensin-converting Enzyme (ACE) MCF7 cells Cyclin dependent kinase inhibit CHI3L1 ovarian cancer BMS265246 Calu-3 cells BMS 265246 COVID-19 inhibitor

 

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