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BMS-265246 | BMS-265246 : ATP competitive inhibitor of CDK1, CDK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK1
  • IC 50:6 nM
  • EC 50:293-492 nM
CDK2
  • IC 50:9 nM
  • EC 50:293-492 nM
ATP competitive
Up to 50 nM

Selectivity

Potency
Cellular
In Vitro

CDK1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-10-0720

CDK2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-10-0720

Chemical Information

Molecular Formula C18H17F2N3O2
SMILEs CCCCOc1c(C(=O)c2c(F)cc(C)cc2F)c[nH]c2nncc1-2
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)
Molecular weight 345.13 Da
AlogP 3.9060200000000025
HBond acceptors 5
HBond donors 1
Atoms 42

References

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Expert Reviews

by SERP
(on 18 Jun 2016 )
Cellular Use Rating
In Model Organisms
Although BMS-265246 is shown (in Bioorg Med Chem Lett 2003, 13, 2405-2408) to be a potent inhibitor of CDK1 (IC50 6 nM) and CDK2 (9 nM) with selectivity over CDK4 (230 nM), no broader kinase selectivity...
by SERP
(on 19 Jun 2016 )
Cellular Use Rating
This compound has limited aqueous solubility: water < 1mg/mL; ethanol < 1mg/mL; DMSO 20mg/mL. Selectivity for CDK1 and CDK2 over CDK4 was 38-fold and 25-fold, respectively. In the ovarian cancer cell...
by SERP
(on 15 Jun 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
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