BMS-265246 Chemical Properties

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

BMS-265246 Usage And Synthesis

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]

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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