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Cat. No. Name Size Price Add Cart
KI3475BMS-265246QuoteQuote

Chemical Characteristic

Product NameBMS-265246
CAS No.582315-72-8
Molecular Weight 345.34
FormulaC18H17F2N3O2
Chemical Name(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)methanone
SmilesC(=O)(c1c(cc(cc1F)C)F)c1c(c2c(nc1)[nH]nc2)OCCCC
Chemical Structure

Biological activities

BMS-265246 is a selective Cyclin-dependent kinase 1/2 (CDK1/2) inhibitor. In vitro, BMS-265246 inhibits the activity of CDK1/2 with IC50s of 6 and 9nM, respectively.[1] BMS-265246 produces a cytotoxic effect with an IC50 of 0.76µM in an ovarian cancer cell line A2780. BMS-265246 exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent, respectively than phenyl analogue. BMS-265246 represents the most potent CDK/CDK2 selective inhibitor from this chemotype. Another in vitro test shows that the dominant cell populations are G2-arrested cells having 4n DNA content, large round nuclei, and low DNA intensity after treatment with BMS-265246 in HCT-116 cells.[1]

Protocols

BMS-265246 is dissolved in 2% DMSO in vitro.[2]

References

[1] Misra RN, Xiao Hy, Rawlins DB, Shan W, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003, 13(14):2405-2408.
[2] Kim KS, Kimball SD, Misra RN, et, al. Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2002, 45(18):3905-3927.

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Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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