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Barasertib (AZD1152-HQPA)

Name: Barasertib (AZD1152-HQPA)
Brand: Selleck Chemicals
SKU: S1147
Rating: 5 (149 reviews)

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

Catalog No.S1147 Purity:99.97%

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

CAS No. 722544-51-6

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Barasertib (AZD1152-HQPA) Related Products

Related Targets	Aurora A Aurora B Aurora C Aurora B	Click to Expand
Related Products	Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Hesperadin Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 SNS-314 CCT137690 GSK1070916 CYC116 TAK-901 CCT129202 SNS-314 Mesylate LY3295668 SP-96	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

Aurora Kinase Signaling Pathway

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

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02579226	Completed	Advanced Solid Tumours	AstraZeneca	October 28 2015	Phase 1

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
	Clear solution	5% DMSO 1 95% corn oil	0.65mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	2.5mg/ml (4.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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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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