| Identification | Back Directory | [Name]
BMS-265246 | [CAS]
582315-72-8 | [Synonyms]
CS-984
BMS-265246
BMS-265246, >=98%
BMS-265246 USP/EP/BP
BMS265246; BMS 265246
(4-Butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)-methanone
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 BMS265246 | [Molecular Formula]
C18H16F2N3O2 | [MDL Number]
MFCD22420825 | [MOL File]
582315-72-8.mol | [Molecular Weight]
344.335 |
| Chemical Properties | Back Directory | [Boiling point ]
552.9±50.0 °C(Predicted) | [density ]
1.304±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥17.25 mg/mL in DMSO | [form ]
solid | [pka]
8.50±0.40(Predicted) | [color ]
White to pink | [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) | [InChIKey]
SCFMWQIQBVZOQR-UHFFFAOYSA-N | [SMILES]
C(C1=CN=C2NN=CC2=C1OCCCC)(C1=C(F)C=C(C)C=C1F)=O |
| Hazard Information | Back Directory | [Uses]
BMS-265246 is a potent and selective pyra-zolopyridine based inhibitor of cdk2/cyclinE, cdk1/cyclinB and cdk4/ cyclinD. | [Biological Activity]
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] | [Enzyme inhibitor]
This cyclin -directed inhibitor (FW = 345.34 g/mol; CAS 582315-72-8;
Solubility: 20 mg/mL DMSO; <1 mg/mL Water), also known systematically
as (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl) (2,6-difluoro-4-methylphenyl)
methanone, targets CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM
and 9 nM, respectively. Cyclin Target Selectivity: Cdk1 (+++), Cdk2 (+++),
Cdk3 (weak, if any), Cdk4 (+), Cdk5 (weak, if any), Cdk6 (weak, if any),
Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10
(weak, if any). | [IC 50]
CDK1/cycB: 6 nM (IC50); CDK2/Cyc E: 9 nM (IC50); CDK4/cycD: 230 nM (IC50) | [storage]
Store at -20°C | [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. bioorgmed 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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