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Barasertib (AZD1152-HQPA)

Catalog No. S1147 5 5 5 Customer Review(s) Product Citations7 Product Citation(s)
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Barasertib (AZD1152-HQPA) Chemical Structure

Bio Information

Barasertib (AZD1152-HQPA) is a highly potent and selective Aurora B inhibitor with a Ki of 0.36 nM. Barasertib (AZD1152-HQPA) inhibits Aurora A with a Ki of 1.37 nM. AZD1152 is converted rapidly to the active Barasertib (AZD1152-HQPA) in plasma. Barasertib (AZD1152-HQPA) has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of Barasertib (AZD1152-HQPA) to tumor cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis. [1][2][3]

References:

[1] Journal of Hepatology 2010;52：63–71

[3] Oncogene 2008;27：3244–3255

[2] haematologica 2008;93(5) ：662－669

Chemical Information

Molecular Weight (WM): 507.56
Formula:

C26H30FN7O3
Solubility(R.T.:25°C): DMSO 102mg/mL 
Water <1mg/mL 
Ethanol 3mg/mL 

Quality Control

View current batch:
H-NMR HPLC

Research Area

Cell Cycle >> Aurora Kinase >> Aurora Kinase Inhibitors

Recommended Screening Libraries

Related Inhibitors

Information  
VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.
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MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM.
  • 5mg
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  • 10mg
  • $ 320
ZM-447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively.
  • 5mg
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Danusertib (PHA-739358) is an Aurora inhibitor for Aurora A/B/C, Bcr-Abl, c-RET and FGFR with IC50 of 13 nM/79 nM/61 nM, 25 nM, 31 nM and 47 nM, respectively.
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MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM.
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Related Antibodies

Information  
Reactivity: 薛亚红

Barasertib (AZD1152-HQPA) has been referenced in 7 publications.

A complex of Kif18b and MCAK promotes microtubule depolymerization and is negatively regulated by Aurora kinases.
System-level analysis of neuroblastoma tumor-initiating cells implicates AURKB as a novel drug target for neuroblastoma.
The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent.
Aurora B interacts with NIR-p53, leading to p53 phosphorylation in its DNA-binding domain and subsequent functional suppression.
Localized Aurora B activity spatially controls non-kinetochore microtubules during spindle assembly.
Aurora kinase B/C inhibition impairs malignant glioma growth in vivo.
Canine osteosarcoma cells exhibit resistance to aurora kinase inhibitors.

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Average Customer Review

(5 customer reviews)

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  • ;J Pharmacol Exp Ther, 2012, 343(3), 617-27
    Barasertib (AZD1152-HQPA) purchased from Selleck


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  • ;Oncogene, 2012, 31, 1217–1227
    Barasertib (AZD1152-HQPA) purchased from Selleck


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  • Data from [Clin Cancer Res 2010;16, 4572-4582]
    Barasertib (AZD1152-HQPA) purchased from Selleck


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  • Data from [J Biol Chem 2011;286, 2236-44]
    Barasertib (AZD1152-HQPA) purchased from Selleck


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  • ;Dr Gao Zhang of University of Pennsylvania
    Barasertib (AZD1152-HQPA) purchased from Selleck

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;J Pharmacol Exp Ther, 2012, 343(3), 617-27


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;Oncogene, 2012, 31, 1217–1227

+ See All 5 Customer Reviews of Barasertib (AZD1152-HQPA)

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