Barasertib (AZD1152-HQPA)

Synonyms: AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib

Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

Barasertib (AZD1152-HQPA) Chemical Structure

Barasertib (AZD1152-HQPA) Chemical Structure

CAS No. 722544-51-6

Purity & Quality Control

Barasertib (AZD1152-HQPA) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCaP Growth Inhibition Assay 0-500 nM 48 h IC50=25 nM 25277659
LNCaP Apoptosis Assay 0-500 nM 48 h induces apoptotic cell death through caspase-3 upregulation 25277659
LNCaP Function Assay 50 nM 48 h induces micronuclei with aneugenic mechanism 25277659
Ramos Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
Daudi  Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
L540 Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
BJAJ Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
Ramos Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
Raji Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
Daudi  Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
L428 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
KM-H2 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
HDLM-2 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
L450 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
BJAJ Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Ramos Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Raji Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Daudi  Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
L428 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
KM-H2 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
HDLM-2 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
L450 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
SW620 Growth Inhibition Assay EC50=10±2.1 nM 21245090
HCT116 Growth Inhibition Assay EC50=11±3.3 nM 21245090
MDA-MB-435 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=125 nM 20175926
MDA-MB-468 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=14 nM 20175926
MDA-MB-231 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=105 nM 20175926
BT474 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=8 nM 20175926
MDA-MB-361 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=70 nM 20175926
HER18 Growth Inhibition Assay 0-10000 nM 2-5 d DMSO IC50=20 nM 20175926
HER18 Apoptosis Assay 100 nM 0/24/48 h DMSO induces apoptosis and reduces clonogenic potential 20175926
MDA-MB-231 Apoptosis Assay 105 nM 0/24/48 h DMSO induces apoptosis and reduces clonogenic potential 20175926
JHH-1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=17.4±1.0 nM 19913935
JHH-2 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=218.0±10.8 nM 19913935
JHH-4 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=155.6±16.8 nM 19913935
HuH-1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=27.3±5.0 nM 19913935
HuH-6 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=3.7±0.6 nM 19913935
HuH-7 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=6.8±0.3 nM 19913935
HLE Growth Inhibition Assay 0.3–1000 nM 72 h EC50=45.9±6.4 nM 19913935
HLF Growth Inhibition Assay 0.3–1000 nM 72 h EC50=126.1±12.2 nM 19913935
PLC/PRF/5 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=76.9±9.9 nM 19913935
SK-Hep1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=21.9±1.2 nM 19913935
Hep3B Growth Inhibition Assay 0.3–1000 nM 72 h EC50=7.6±1.2 nM 19913935
HepG2 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=14.7±1.7 nM 19913935
Ramos Apoptosis Assay 25/50/100 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
Daudi  Apoptosis Assay 25/50/100 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
BALM-14 Apoptosis Assay 12.5/25/50 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
BALM-27 Apoptosis Assay 12.5/25/50 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
NB4 Growth Inhibition Assay 0.01/0.1/1 μM 48 h inhibits cell growth significantly 18367484
HeLa Function Assay 1 uM 24 hrs Inhibition of aurora B autophosphorylation in human HeLa cells at 1 uM after 24 hrs by Western blotting 20684549
Click to View More Cell Line Experimental Data

Biological Activity

Description Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Targets
Aurora B [1]
(Cell-free assay)
0.37 nM
In vitro
In vitro

Barasertib (AZD1152-HQPA), a highly selective Aurora B inhibitor, causes polyploidy and apoptosis in many cancer cell lines.[1]

Cell Research Cell lines NCI-H82 cells, SCLC and NSCLC cell lines
Concentrations --
Incubation Time --
Method

--

Experimental Result Images Methods Biomarkers Images PMID
Western blot AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN p53 / p21 / p-p38 / p38 26497213
Immunofluorescence p21 24782314
Growth inhibition assay Cell viability 26497213
In Vivo
In vivo

Barasertib (AZD1152-HQPA) is an aurora B kinase inhibitor, and has efficacy against RB1 / SCLC cell line xenografts, RB1 / SCLC PDXs, and autochthonous Rb1 / neuroendocrine tumors.[1]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02579226 Completed
Advanced Solid Tumours
AstraZeneca
October 28 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 507.56 Formula

C26H30FN7O3

CAS No. 722544-51-6 SDF Download Barasertib (AZD1152-HQPA) SDF
Smiles CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (197.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Can you let me know what solvent I can use for Barasertib, cat # S1147, for in vivo use? (IP injection in mice)

Answer:
S1147 Barasertib (AZD1152-HQPA) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

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