BMS-265246
Modify Date: 2024-01-11 00:37:49
BMS-265246 structure
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Common Name | BMS-265246 | ||
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| CAS Number | 582315-72-8 | Molecular Weight | 345.343 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 552.9±50.0 °C at 760 mmHg | |
| Molecular Formula | C18H17F2N3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 288.2±30.1 °C | |
Use of BMS-265246BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively. IC50 Value: 6 nM(for CDK1/cyclin B); 9 nM(for CDK2/cyclin E)Target: CDK1/2in vitro: BMS-265246 inhibits the activity of Cdk4/cycD (IC50 = 0.23 μM) and prevents A2780 Cytox with IC50 of 0.76 μM. BMS-265246 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. BMS-265246 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.in vivo: |
| Name | (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone |
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| Synonym | More Synonyms |
| Description | BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively. IC50 Value: 6 nM(for CDK1/cyclin B); 9 nM(for CDK2/cyclin E)Target: CDK1/2in vitro: BMS-265246 inhibits the activity of Cdk4/cycD (IC50 = 0.23 μM) and prevents A2780 Cytox with IC50 of 0.76 μM. BMS-265246 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. BMS-265246 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.in vivo: |
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| Related Catalog | |
| Target |
CDK1/cycB:6 nM (IC50) CDK2/Cyc E:9 nM (IC50) CDK4/cycD:230 nM (IC50) |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 552.9±50.0 °C at 760 mmHg |
| Molecular Formula | C18H17F2N3O2 |
| Molecular Weight | 345.343 |
| Flash Point | 288.2±30.1 °C |
| Exact Mass | 345.128876 |
| PSA | 67.87000 |
| LogP | 3.51 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.595 |
| Storage condition | -20℃ |
| cs-0922 |
| Methanone, (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)- |
| (4-Butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)methanone |
| unii-4gf4a623rf |
| BMS-265246 |