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AZD1152 | Inhibitor of AURKB
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
AURKB
  • Ki:<1 nM
  • IC50:<1 nM
Inhibitor
Up to 100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - AURKC 17 nM, AURKBA 1.4 uM, LCK 1.7 uM, KDR 1.8 uM, PHK 1.8 uM, ZAP70 8.2 uM

Potency
Cellular
In Vitro

AURKB

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm061335f

In Vivo Validations

Mouse
Dose: 150 mg/kg
Route of delivery: Intravenous, Subcutaneous
Plasma half life: 4.9-5.8 h
Systemic clearance: 14 mg/mL/kg (in rat)
Organ of interest (O): tumor xenograft (SW620 cells)
Target engagement assay: Indirect, protein substrate phosphorylation assay (phospho H3)

DOI Reference: 10.1021/jm061335f

Orthogonal Probes def

AMG900
XMD-12

Chemical Information

Molecular Formula C26H31FN7O6P
SMILEs CCN(CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1)CCOP(=O)(O)O
InChI InChI=1S/C26H31FN7O6P/c1-2-34(10-12-40-41(36,37)38)9-4-11-39-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(35)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17H,2,4,9-12,15H2,1H3,(H,30,35)(H2,36,37,38)(H2,28,29,31,32,33)
Molecular weight 587.21 Da
AlogP 3.6169
HBond acceptors 13
HBond donors 5
Atoms 72

References

Publications

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Vendors

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Expert Reviews

by SERP
(on 31 May 2016 )
Cellular Use Rating
In Model Organisms
AZD1152 is a phosphate pro-drug that is rapidly cleaved to the active alcohol. The active alcohol is a potent inhibitor of AURB and AURC. We have dosed AZD1152 in tumor xenograft models in mice using...
by SERP
(on 7 Jun 2016 )
Cellular Use Rating
In Model Organisms
I would like to see a more comprehensive screen of this probe against more than 50 kinases to confirm its broad selectivity. IC50 is listed at 0.37 nM. It is ~3700-fold more selective for Aurora B over...
by SERP
(on 18 Aug 2016 )
Cellular Use Rating
In Model Organisms
AZD1152 is a phosphate prodrug designed for in vivo studies only. The active form is compound 34 in the corresponding J Med Chem paper, with Aurora B inhibition IC50 <1 nM and the corresponding functional...
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