BMS265246CDK1/2 inhibitor,potent and selective CAS# 582315-72-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 582315-72-8 | SDF | Download SDF |
| PubChem ID | 5329775 | Appearance | Powder |
| Formula | C18H17F2N3O2 | M.Wt | 345.34 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone | ||
| SMILES | CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F | ||
| Standard InChIKey | SCFMWQIQBVZOQR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H17F2N3O2/c1-3-4-5-25-17-11(8-21-18-12(17)9-22-23-18)16(24)15-13(19)6-10(2)7-14(15)20/h6-9H,3-5H2,1-2H3,(H,21,22,23) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent cdk1/2 inhibitor (IC50 values are 6, 9 and 230 nM for cdk1, cdk2 and cdk4, respectively). Inhibits proliferation of HCT-116 colon cancer cells in vitro. |
BMS265246 Dilution Calculator
BMS265246 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8957 mL | 14.4785 mL | 28.957 mL | 57.9139 mL | 72.3924 mL |
| 5 mM | 0.5791 mL | 2.8957 mL | 5.7914 mL | 11.5828 mL | 14.4785 mL |
| 10 mM | 0.2896 mL | 1.4478 mL | 2.8957 mL | 5.7914 mL | 7.2392 mL |
| 50 mM | 0.0579 mL | 0.2896 mL | 0.5791 mL | 1.1583 mL | 1.4478 mL |
| 100 mM | 0.029 mL | 0.1448 mL | 0.2896 mL | 0.5791 mL | 0.7239 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BMS265246 is a potent and selective inhibitor for CDK1 and CDK2 (IC50= 6 nM and 9 nM)
Cyclin-dependent kinases (CDK) are a group of serine/threonine kinases. They are activated by coupling to cyclin and participate in the regulation of cell cycle.
BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 μM and 0.76 μM) [1]. In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 μm—0.492 μm). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells. [2]
References:
1. Misra RN, Xiao Hy, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg
Med Chem Lett. 2003 Jul 21;13(14):2405-8.
2. Sutherland JJ, Low J, Blosser W et al. A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.
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1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.[Pubmed:12824044]
Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.
Structure-activity studies of 1H-pyrazolo[3,4-b]pyridine 1 have resulted in the discovery of potent CDK1/CDK2 selective inhibitor 21h, BMS-265246 (CDK1/cycB IC(50)=6 nM, CDK2/cycE IC(50)=9 nM). The 2,6-difluorophenyl substitution was critical for potent inhibitory activity. A solid state structure of 21j, a close di-fluoro analogue, bound to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone.
