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AZD1152(Barasertib) Aurora Kinase inhibitor

Name: AZD1152(Barasertib)
SKU: S1051
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S1051

AZD1152 (Barasertib) is a selective inhibitor of Aurora B with K_i of 0.36 nM.

Chemical Structure

Molecular Weight: 587.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.684%

99.684

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Chemical Information, Storage & Stability

Molecular Weight	587.54	Formula	C₂₆H₃₁FN₇O₆P	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	722543-31-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (170.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Mechanism of Action

Features	Selectivity for Aurora-B over Aurora-A.
Targets/IC₅₀/Ki	Aurora B ^[1] 0.36 nM
In vitro	AZD1152 (Barasertib) is a pro-drug converting to active substance AZD1152-HQPA in human plasma, which inhibits Aurora-A, Aurora B-INCENP, and Aurora C-INCENP with K_is of 687 nM, 0.36 nM, and 17.0 nM, indicating a 100-fold selectivity for Aurora-B over Aurora-A. ^[1] This compound results in a dose-dependent inhibition of histone H3 phosphorylation on Ser¹⁰ in SW620 colorectal tumor cell line. ^[2] It induces growth arrest of a variety of types of leukemia cells, with IC50 of 5, 12, and 8 nM for ALL PALL-2, MOLM13, MV4-11 respectively. ^[3]
Kinase Assay	Affinity determination
Kinase Assay	AZD1152 (Barasertib) is incubated with Aurora A or Aurora B-INCENP and the substrate peptide. Twenty microliters of reaction mix (25 mM Tris-HCl, 12.7 mM KCl, 2.5 mM NaF, 0.6 mM dithiothreitol, 6.25 mM MnCl₂, 7.5μM ATP for Aurora A assay and 15 μM for Aurora B-INCENP assay, 6.25 μM peptide substrate containing 0.2 μCi [γ³³P]ATP) is then added to all test wells to start the reaction (to give a final volume of 50 μL). Plates are incubated at room temperature for 60 min, reactions are stopped by addition of 100 μL of 20% v/v orthophosphoric acid, and peptide substrate is captured on positively charged nitrocellulose P30 filtermat using a 96-well plate harvester and then assayed for incorporation of ³³P with a Beta plate counter.
In vivo	AZD1152 (Barasertib) (2.5 mg/kg/d) significantly suppresses PhH3 by 69% in SW620 colon tumors. It (10-150 mg/kg/d) inhibits growth in a panel of human tumor xenografts including Colo205, A549, and HL-60 with inhibition rate ranging from 55% to 100%. Additional results show cells exposed to this compound end up apoptosis.^[2] It (25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors in MOLM13 xenografts.^[3]
References	[1] http://www.aacr.org/home/scientists/meetings--workshops/molecular-targets-and-cancer-therapeutics/previous-molecular-targets-and-cancer-therapeutics-conferences/2005-molecular-targets-and-cancer-therapeutics/proceedings.aspx [2] http://www.ncbi.nlm.nih.gov/pubmed?term=17575233 [3] http://www.ncbi.nlm.nih.gov/pubmed?term=17495131 [4] http://www.ncbi.nlm.nih.gov/pubmed?term=17373783

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